Dexamethasone
别名: NSC 34521, Hexadecadrol, Prednisolone F,MK-125 中文名称：地塞米松
此产品请避光密封保存。
Dexamethasone是一种有效的半合成的糖皮质激素类甾体药物，也是一种interleukin receptor调节剂，具有抗炎和免疫抑制作用。Dexamethasone 可诱导自噬和线粒体自噬。Dexamethasone 被用于COVID-19临床病人测试中，并发现对危重症患者有一定效果。
Dexamethasone Chemical Structure
CAS: 50-02-2
产品质控
批次：
S132205
DMSO]200 mg/mL]false]Ethanol]20 mg/mL]false]Water]Insoluble]false
纯度：
99.39%
99.39
常与Dexamethasone一起在实验中被使用的化合物
Dexamethasone和Pomalidomide治疗复发或难治性多发性骨髓瘤的临床试验仍在进行中。
Dexamethasone和Bortezomib的使用为多发性骨髓瘤(MM)的一线治疗提供了高效且耐受性良好的方案。
Hassan Zafar MS, et al. South Asian J Cancer. 2018;7(1):58-60.
Dexamethasone和Venetoclax联合治疗可在PDX模型中诱导长期无白血病生存。
Dexamethasone和Lenalidomide在体外和随机III期临床试验中均表现出有效的抗MM活性。
Hideshima T, et al. Ther Clin Risk Manag. 2008;4(1):129-136.
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| mouse thymocytes | Function assay | 1 μM | 24 h | Induction of apoptosis in mouse thymocytes assessed as internucleosomal DNA fragmentation at 1 uM after 24 hrs by agarose gel electrophoresis | 24794748 |
| human monocytes | Function assay | 5 μM | 20 h | Antiinflammatory activity in human monocytes assessed as inhibition of LPS-induced COX2 expression at 5 uM after 20 hrs using rabbit polyclonal antibody IgG by SDS-PAGE analysis | 21843935 |
| R1 | Function assay | 10 uM | 24 hrs | Inhibition of glucocorticoid receptor-glucocorticoid complex transfected in rat R1 cells assessed as down-regulation of TPA-responsive element proinflammatory gene expression at 10 uM after 24 hrs by beta-galactosidase assay, IC50 = 0.005 μM. | 18412397 |
| NIH-3T3 | Function assay | 0.01 mg/kg | 1 hr | Plasma concentration in mouse bearing mouse NIH-3T3 cells integrated with MMTV reporter gene at 0.01 mg/kg, po after 1 hr, Cp = 0.044 μM. | 20469868 |
| NIH-3T3 | Function assay | 0.1 mg/kg | 1 hr | Plasma concentration in mouse bearing mouse NIH-3T3 cells integrated with MMTV reporter gene at 0.1 mg/kg, po after 1 hr, Cp = 0.236 μM. | 20469868 |
| NIH-3T3 | Function assay | 1 mg/kg | 1 hr | Plasma concentration in mouse bearing mouse NIH-3T3 cells integrated with MMTV reporter gene at 1 mg/kg, po after 1 hr, Cp = 1.8 μM. | 20469868 |
| NIH-3T3 | Function assay | 10 mg/kg | 1 hr | Plasma concentration in mouse bearing mouse NIH-3T3 cells integrated with MMTV reporter gene at 10 mg/kg, po after 1 hr, Cp = 17.7 μM. | 20469868 |
| NIH-3T3 | Function assay | 0.01 mg/kg | 1 hr | Fraction unbound in mouse plasma bearing mouse NIH-3T3 cells integrated with MMTV reporter gene at 0.01 mg/kg, po after 1 hr, Fu = 0.00203 μM. | 20469868 |
| NIH-3T3 | Function assay | 0.1 mg/kg | 1 hr | Fraction unbound in mouse plasma bearing mouse NIH-3T3 cells integrated with MMTV reporter gene at 0.1 mg/kg, po after 1 hr, Fu = 0.0116 μM. | 20469868 |
| NIH-3T3 | Function assay | 1 mg/kg | 1 hr | Fraction unbound in mouse plasma bearing mouse NIH-3T3 cells integrated with MMTV reporter gene at 1 mg/kg, po after 1 hr, Fu = 0.087 μM. | 20469868 |
| NIH-3T3 | Function assay | 10 mg/kg | 1 hr | Fraction unbound in mouse plasma bearing mouse NIH-3T3 cells integrated with MMTV reporter gene at 10 mg/kg, po after 1 hr, Fu = 5.123 μM. | 20469868 |
| RAW264.7 | Antiinflammatory assay | 10 uM | 24 hrs | Antiinflammatory activity in LPS-stimulated mouse RAW264.7 cells assessed as nitrite level at 10 uM after 24 hrs by Griess method, Activity = 1.54 μM. | 21353543 |
| A549 | Antiinflammatory assay | 1 uM | 30 mins | Antiinflammatory activity in human A549 cells assessed as inhibition of IL-1beta-induced mPGES1 expression at 1 uM treated 30 mins prior to IL-1beta challenge measured after 48 hrs by Western blot analysis relative to control | 22795900 |
| IOBA-NHC | Function assay | 40 uM | 24 hrs | Inhibition of NF-kappaB p65-mediated IL-6 release in HSV1 KOS infected human IOBA-NHC cells at 40 uM after 24 hrs by ELISA | 23219855 |
| IOBA-NHC | Function assay | 40 uM | 24 hrs | Inhibition of NF-kappaB p65-mediated TNFalpha release in HSV1 KOS infected human IOBA-NHC cells at 40 uM after 24 hrs by ELISA | 23219855 |
| IOBA-NHC | Function assay | 40 uM | 24 hrs | Inhibition of NF-kappaB p65-mediated IL-8 release in HSV1 KOS infected human IOBA-NHC cells at 40 uM after 24 hrs by ELISA | 23219855 |
| HCLE | Function assay | 40 uM | 24 hrs | Inhibition of NF-kappaB p65-mediated IL-8 release in HSV1 KOS infected human HCLE cells at 40 uM after 24 hrs by ELISA | 23219855 |
| HCT116 | Function assay | 20 to 40 uM | 24 hrs | Agonist activity at glucocorticoid receptor (unknown origin) expressed in human HCT116 cells co-expressing GRE at 20 to 40 uM after 24 hrs by luciferase reporter gene assay | 23276449 |
| B16F10 | Antitumor assay | 20 mg/kg | 24 days | Antitumor activity against mouse B16F10 cells xenografted in C57BL/6 mouse assessed as inhibition tumor growth at 20 mg/kg, ip measured after 24 days of tumor inoculation | 24992071 |
| B16F10 | Antitumor assay | 20 mg/kg | 24 days | Antitumor activity against mouse B16F10 cells xenografted in C57BL/6 mouse assessed as apoptotic regions at 20 mg/kg, ip measured after 24 days of tumor inoculation by TUNEL assay | 24992071 |
| B16F10 | Apoptosis assay | 10 uM | 48 hrs | Induction of apoptosis in mouse B16F10 cells assessed as increase in ratio of BAX/Bcl2 expression at 10 uM after 48 hrs by Western blot analysis relative to untreated control | 24992071 |
| B16F10 | Antitumor assay | 20 mg/kg | 24 days | Antitumor activity against mouse B16F10 cells xenografted in C57BL/6 mouse assessed as apoptotic regions at 20 mg/kg, ip measured after 24 days of tumor inoculation by VE-cadherin | 24992071 |
| RAW264.7 | Antiinflammatory assay | 1 mM | 30 mins | Antiinflammatory activity against mouse RAW264.7 cells assessed as reduction of LPS-induced TNF mRNA expression cells at 1 mM treated 30 mins before LPS challenge measured after 3 hrs by qRT-PCR analysis | 25667960 |
| J774 | Antiinflammatory assay | 10 uM | 24 hrs | Antiinflammatory activity against mouse J774 cells assessed as inhibition of LPS-induced iNOS expression at 10 uM after 24 hrs by Western blot analysis | 26915998 |
| C57BL/6 | Antiinflammatory assay | 10 mg/kg | 1 hr | Antiinflammatory activity in C57BL/6 mouse assessed as inhibition of zymosan-induced mononuclear cells migration in articular cavity at 10 mg/kg, ip administered 1 hr prior to zymosan challenge measured at 6 to 24 hrs | 27227459 |
| C57BL/6 | Antiinflammatory assay | 10 mg/kg | 1 hr | Antiinflammatory activity in C57BL/6 mouse assessed as inhibition of zymosan-induced infiltration of inflammatory cells into synovial tissue at 10 mg/kg, ip administered 1 hr prior to zymosan challenge measured at 6 to 24 hrs by hematoxylin and eosin stai | 27227459 |
| J774A.1 | Antiinflammatory assay | 1 uM | 1 hr | Antiinflammatory activity in mouse J774A.1 cells assessed as inhibition of zymosan and IFNgamma-induced IL6 production in cell-free supernatant at 1 uM preincubated for 1 hr followed by zymosan and IFNgamma addition measured after 24 hrs by sandwich ELISA | 27227459 |
| J774A.1 | Antiinflammatory assay | 1 uM | 1 hr | Antiinflammatory activity in mouse J774A.1 cells assessed as inhibition of zymosan and IFNgamma-induced COX2 expression at 1 uM preincubated for 1 hr followed by zymosan and IFNgamma addition measured after 24 hrs by Western blot analysis | 27227459 |
| J774A.1 | Antiinflammatory assay | 1 uM | 1 hr | Antiinflammatory activity in mouse J774A.1 cells assessed as inhibition of zymosan and IFNgamma-induced nitric oxide production at 1 uM preincubated for 1 hr followed by zymosan and IFNgamma addition measured after 24 hrs by colorimetric Griess test | 27227459 |
| Mino | Antiproliferative assay | 100 uM | 48 hrs | Antiproliferative activity against human Mino cells at 100 uM preincubated for 48 hrs followed by thymidine addition measure after 16 hrs by Thymidine incorporation assay | 28858511 |
| RAW264.7 | Function assay | 10 uM | 1 hr | Agonist activity at PPARgamma in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of NF-kappaB signaling by measuring reduction in COX2 mRNA level at 10 uM pretreated with compound for 1 hr followed by LPS stimulation for 6 hrs by RT-PCR analysi | 29389121 |
| RAW264.7 | Function assay | 10 uM | 1 hr | Agonist activity at PPARgamma in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of NF-kappaB signaling by measuring reduction in iNOS mRNA level at 10 uM pretreated with compound for 1 hr followed by LPS stimulation for 6 hrs by RT-PCR analysi | 29389121 |
| RAW264.7 | Function assay | 10 uM | 1 hr | Agonist activity at PPARgamma in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of NF-kappaB signaling by measuring reduction in TNFalpha mRNA level at 10 uM pretreated with compound for 1 hr followed by LPS stimulation for 6 hrs by RT-PCR ana | 29389121 |
| RAW264.7 | Function assay | 10 uM | 1 hr | Agonist activity at PPARgamma in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of NF-kappaB signaling by measuring reduction in IL-1beta mRNA level at 10 uM pretreated with compound for 1 hr followed by LPS stimulation for 6 hrs by RT-PCR ana | 29389121 |
| RAW264.7 | Function assay | 10 uM | 1 hr | Agonist activity at PPARgamma in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of NF-kappaB signaling by measuring reduction in IL-6 mRNA level at 10 uM pretreated with compound for 1 hr followed by LPS stimulation for 6 hrs by RT-PCR analysi | 29389121 |
| RAW264.7 | Function assay | 10 uM | 1 hr | Agonist activity at PPARgamma in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of NF-kappaB signaling by measuring reduction in NO production at 10 uM pretreated with compound for 1 hr followed by LPS stimulation measured after 24 hrs by Grie | 29389121 |
| RAW264.7 | Function assay | 10 uM | 1 hr | Agonist activity at PPARgamma in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of NF-kappaB signaling by measuring reduction in IL-1beta production at 10 uM pretreated with compound for 1 hr followed by LPS stimulation measured after 24 hrs b | 29389121 |
| RAW264.7 | Function assay | 10 uM | 1 hr | Agonist activity at PPARgamma in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of NF-kappaB signaling by measuring reduction in IL-6 production at 10 uM pretreated with compound for 1 hr followed by LPS stimulation measured after 24 hrs by EL | 29389121 |
| RAW264.7 | Function assay | 10 uM | 1 hr | Agonist activity at PPARgamma in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of NF-kappaB signaling by measuring reduction in TNFalpha production at 10 uM pretreated with compound for 1 hr followed by LPS stimulation measured after 3 hrs by | 29389121 |
| RAW264.7 | Function assay | 10 uM | 1 hr | Agonist activity at PPARgamma in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of NF-kappaB signaling by measuring reduction in iNOS protein level at 10 uM pretreated with compound for 1 hr followed by LPS stimulation measured after 24 hrs by | 29389121 |
| HeLa | Function assay | 0.4 uM | 24 hrs | Transrepression of GCR in human HeLa cells assessed as suppression of DEX-induced GILZ mRNA expression at 0.4 uM after 24 hrs by Taqman-based real-time PCR analysis | 29670697 |
| RAW264.7 | Antiinflammatory assay | 20 uM | 6 hrs | Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced IL-6 production at 20 uM pretreated for 6 hrs followed by LPS stimulation measured after 24 hrs by ELISA | 30215255 |
| RAW264.7 | Antiinflammatory assay | 20 uM | 6 hrs | Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced IL-1beta production at 20 uM pretreated for 6 hrs followed by LPS stimulation measured after 24 hrs by ELISA | 30215255 |
| RAW264.7 | Antiinflammatory assay | 20 uM | 6 hrs | Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced nitrite production at 20 uM pretreated for 6 hrs followed by LPS stimulation measured after 24 hrs by ELISA | 30215255 |
| RAW264.7 | Antiinflammatory assay | 20 uM | 6 hrs | Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced TNFalpha production at 20 uM pretreated for 6 hrs followed by LPS stimulation measured after 24 hrs by ELISA | 30215255 |
| A549 | Function assay | 10 uM | Antagonist activity for Glucocorticoid receptor in MMTV transactivation assay in human A549 lung epithelial cells at 10 uM, IC50 = 10 μM. | 15999989 | |
| COS7 | Function assay | 1 uM | Agonist activity at glucocorticoid receptor Q570A mutant in COS7 cells at 1 uM by NF-kappaB-luciferase reporter gene assay | 18038970 | |
| RAW264.7 | Function assay | 10 uM | Inhibition of LPS-stimulated COX2 expression in mouse RAW264.7 cells at 10 uM by Western blot | 18790649 | |
| RAW264.7 | Function assay | 2 hrs | Inhibition of mPGES1 expression in LPS-stimulated mouse RAW264.7 cells after 2 hrs by Western blot analysis | 17407277 | |
| RAW264.7 | Function assay | 2 hrs | Inhibition of COX2 expression in LPS-stimulated mouse RAW264.7 cells after 2 hrs by Western blot analysis | 17407277 | |
| RAW 264.7 | Function assay | 24 hrs | Inhibition of interferon gamma-stimulated NO production in RAW 264.7 cells after 24 hrs, IC50 = 0.02 μM. | 17367124 | |
| RAW264.7 | Antiinflammatory assay | 24 hrs | Antiinflammatory activity in LPS-stimulated mouse RAW264.7 cells assessed as effect on TNFalpha formation pretreated 1 hr before LPS challenge measured after 24 hrs, IC50 = 0.7 μM. | 11908984 | |
| rat polymorphonuclear leukocytes | Function assay | 20 mins | Antiinflammatory activity in rat polymorphonuclear leukocytes assessed as inhibition of LPS-stimulated nitric oxide production after 20 mins by Griess method, IC50=2.3 nM | 22506620 | |
| RPMI8226 | Antiproliferative assay | 4 days | Antiproliferative activity against human RPMI8226 cells after 4 days, IC50 = 0.0065 μM. | 17705362 | |
| TH2 | Function assay | 48 hrs | Inhibition of pro-inflammatory cytokine IL5 production in ovalbumin-stimulated BALB/c mouse TH2 cells after 48 hrs by sandwich-ELISA, IC50 = 0.005 μM. | 19323483 | |
| TH2 | Function assay | 48 hrs | Inhibition of pro-inflammatory cytokine IL13 production in ovalbumin-stimulated BALB/c mouse TH2 cells after 48 hrs by sandwich-ELISA, IC50 = 0.005 μM. | 19323483 | |
| A549 | Function assay | 6 hrs | Transrepression activity at glucocorticoid receptor expressed in human A549 cells assessed as inhibition of IL-1-beta-induced NF-kappaB dependent E-selection promoter activation after 6 hrs by luciferase reporter gene based ELAM assay, EC50 = 0.0011 μM. | 20047280 | |
| A549 | Function assay | 6 hrs | Transrepression activity at glucocorticoid receptor expressed in human A549 cells assessed as inhibition of PMA-induced AP1 activity after 6 hrs by luciferase reporter gene assay, EC50 = 0.0025 μM. | 20047280 | |
| U2OS | Function assay | 18 hrs | Agonist activity at glucocorticoid receptor-LBD in human U2OS cells transfected with Gal4-DBD assessed as increase of transactivation activity after 18 hrs by luciferase reporter gene assay, EC50 = 15.8489 μM. | 20812681 | |
| U2OS | Function assay | 18 hrs | Antagonist activity at glucocorticoid receptor-LBD in human U2OS cells transfected with Gal4-DBD assessed as inhibition of transactivation activity after 18 hrs by luciferase reporter gene assay, IC50 = 0.0005082 μM. | 20812681 | |
| HepG2 | Function assay | 24 hrs | Activation of rat PXR expressed in human HepG2 cells after 24 hrs by luciferase reporter gene based luminescent analysis, EC50 = 2.6 μM. | 20966043 | |
| 13D3/Huh7 | Function assay | 24 hrs | Transactivation activity at glucocorticoid receptor in human 13D3/Huh7 cells assessed as induction of tyrosine aminotransferase activity after 24 hrs, EC50 = 0.005 μM. | 21073190 | |
| RAW264.7 | Antiinflammatory assay | 18 hrs | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production treated 2 hrs before LPS challenge measured after 18 hrs by griess reaction, IC50 = 0.86 μM. | 21288727 | |
| HMC1 | Function assay | 1 hr | Immunomodulatory activity in human HMC1 cells assessed as inhibition of phorbol 12-myristate 13-acetate/A23187-stimulated IL1-beta secretion treated 1 hr prior to 30 mins phorbol 12-myristate 13-acetate/A23187 challenge by Western blotting analysis | 21302967 | |
| RAW264.7 | Antiinflammatory assay | 18 hrs | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced TNF-alpha secretion after 18 hrs, IC50 = 0.01 μM. | 21353543 | |
| RAW264.7 | Antiinflammatory assay | 24 hrs | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production after 24 hrs by Griess method, IC50 = 0.8 μM. | 21353543 | |
| RAW264.7 | Antiinflammatory assay | 24 hrs | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of IFN-gamma induced NO production after 24 hrs by Griess reaction, IC50 = 0.02 μM. | 21361338 | |
| RAW264.7 | Function assay | 20 mins | Inhibition of LPS-induced nitric oxide production in mouse RAW264.7 cells pre-incubated for 20 mins before LPS challenge measured 18 hrs post LPS challenge by Griess method | 21775152 | |
| RAW264.7 | Function assay | 30 mins | Inhibition of LPS-induced TNFalpha production in mouse RAW264.7 cells pre-incubated for 30 mins before LPS challenge measured 6 hrs post LPS challenge by ELISA | 21775152 | |
| RAW264.7 | Antiinflammatory assay | 2 hrs | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-stimulated nitric oxide production pretreated for 2 hrs before LPS challenge measured after 18 hrs by Griess method, IC50 = 0.47 μM. | 22372956 | |
| RAW264.7 | Antiinflammatory assay | 2 hrs | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production pretreated for 2 hrs before LPS challenge measured after 18 hrs by Griess method, IC50 = 0.98 μM. | 22537362 | |
| H13 | Function assay | 3 hrs | Inhibition of glucocorticoid receptor in human H13 cells assessed as inhibition of glucocorticoid-induced cell proliferation after 3 hrs by [3H]-thymidine incorporation assay, EC50 = 0.0097 μM. | 23199485 | |
| 293 MSR | Function assay | 60 mins | Displacement of [3H]-dexamethasone human glucocorticoid receptor alpha expressed in 293 MSR cells after 60 mins by scintillation counting, EC50 = 0.0125 μM. | 23199485 | |
| RAW264.7 | Antiinflammatory assay | 2 hrs | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production incubated for 2 hrs prior to LPS-challenge measured after 24 hrs by Griess method, IC50 = 1.43 μM. | 23373965 | |
| HeLaS3 | Function assay | 2 hrs | Displacement of [3H]Dexamethasone from glucocorticoid receptor in human HeLaS3 cells after 2 hrs, IC50 = 0.0041 μM. | 23403082 | |
| HeLaS3 | Function assay | 2 hrs | Displacement of [3H]Dexamethasone from glucocorticoid receptor in human HeLaS3 cells after 2 hrs, Ki = 0.0022 μM. | 23403082 | |
| CUTLL1 | Growth inhibition assay | 48 hrs | Growth inhibition of human CUTLL1 cells with high GR expression levels after 48 hrs by alamar blue assay | 25050160 | |
| RAW264.7 | Function assay | 24 hrs | Inhibition of LPS-induced nitric oxide production in mouse RAW264.7 cells after 24 hrs by Griess assay relative to vehicle-treated control, IC50 = 0.8 μM. | 25499882 | |
| SW1353 | Function assay | 24 hrs | Transrepression activity at glucocorticoid receptor in human SW1353 cells assessed as repression of IL-1-induced MMP-13 production after 24 hrs by ELISA, IC50 = 0.0018 μM. | 25706100 | |
| RAW264.7 | Function assay | 6 hrs | Inhibition of TNFalpha production in mouse RAW264.7 cells incubated for 6 hrs by sandwich immunoassay, IC50 = 0.04 μM. | 25824662 | |
| J774A.1 | Function assay | 6 hrs | Inhibition of TNFalpha production in mouse J774A.1 cells incubated for 6 hrs by sandwich immunoassay, IC50 = 0.4 μM. | 25824662 | |
| RAW264.7 | Function assay | 12 hrs | Inhibition of IL-1beta production in mouse RAW264.7 cells incubated for 12 hrs by sandwich immunoassay, IC50 = 4.7 μM. | 25824662 | |
| J774A.1 | Function assay | 12 hrs | Inhibition of IL-1beta production in mouse J774A.1 cells incubated for 12 hrs by sandwich immunoassay, IC50 = 22 μM. | 25824662 | |
| RAW264.7 | Antiinflammatory assay | 24 hrs | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production after 24 hrs by Griess assay, IC50 = 0.63 μM. | 26087384 | |
| BV2 | Antiinflammatory assay | 24 hrs | Antiinflammatory activity in C57BL6/J mouse BV2 cells assessed as inhibition of LPS-induced nitric oxide production after 24 hrs by Griess assay, IC50 = 0.025 μM. | 26110443 | |
| RAW264.7 | Function assay | 24 hrs | Inhibition of LPS-induced nitric oxide production in mouse RAW264.7 cells after 24 hrs by Griess assay, IC50 = 0.8 μM. | 26305406 | |
| RAW264.7 | Antiinflammatory assay | 24 hrs | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production after 24 hrs in presence of LPS by Griess assay, IC50 = 0.63 μM. | 27825545 | |
| RAW264.7 | Antiinflammatory assay | 30 mins | Antiinflammatory activity in mouse RAW264.7 cells assessed as reduction in LPS-induced NO production pretreated for 30 mins followed by LPS stimulation for 24 hrs by Griess assay, IC50 = 7 μM. | 28499733 | |
| RAW264.7 | Function assay | 24 hrs | Inhibition of LPS-induced NO production in mouse RAW264.7 cells after 24 hrs by Griess assay, IC50 = 2.5 μM. | 28598633 | |
| RAW264.7 | Function assay | 24 hrs | Inhibition of LPS-induced nitric oxide production in mouse RAW264.7 cells after 24 hrs by Griess assay, IC50 = 10.7 μM. | 29518326 | |
| HFF | Antiinflammatory assay | Antiinflammatory activity assessed as upregulation of aromatase in HFF cells by transactivation assay, EC50 = 0.002 μM. | 17692519 | ||
| HFF | Antiinflammatory assay | Antiinflammatory activity assessed as inhibition of IL1 stimulated IL6 production in HFF cells by transrepression assay, EC50 = 0.0005 μM. | 17692519 | ||
| A549 | Function assay | Antagonist activity at glucocorticoid receptor in human A549 cells transfected with MMTV luciferase reporter gene assessed as inhibition of dexamethasone-induced activation, IC50 = 1 μM. | 17616395 | ||
| A549 | Function assay | Agonist activity at glucocorticoid receptor in human A549 cells by NF-kappaB transrepression assay, IC50 = 0.001 μM. | 17616395 | ||
| A549 | Function assay | Agonist activity at glucocorticoid receptor in human A549 cells by MMTV transactivation assay, EC50 = 0.00537 μM. | 17616395 | ||
| HFF | Function assay | Inhibition of IL1-stimulated IL6 production in HFF cells, IC50 = 0.00051 μM. | 17181172 | ||
| HeLa | Function assay | Activation of MMTV in HeLa cells measured by luciferase activity, EC50 = 0.017 μM. | 17181172 | ||
| HFF | Function assay | Induction of aromatase activity in HFF cells assessed as production of beta estradiol by aromatase assay, EC50 = 0.0019 μM. | 17181172 | ||
| A549 | Function assay | Agonist activity at GR assessed as NF-kappaB-mediated transrepression of secreted placental alkaline phosphatase gene in human A549 cells, IC50 = 0.001175 μM. | 16821781 | ||
| A549 | Function assay | Agonist activity at GR assessed as MMTV-mediated transactivation of renilla luciferase gene in human A549 cells relative to Dexamethasone, EC50 = 0.005012 μM. | 16821781 | ||
| A549 | Function assay | Activity at glucocorticoid receptor in human A549 cells assessed as effect on GRE promoter response by luciferase reporter assay, EC50 = 0.001 μM. | 16643060 | ||
| RAW 264.7 | Function assay | Inhibitory activity against TNF-alpha release in RAW 264.7 cells in the supernatant, IC50 = 0.42 μM. | 12361395 | ||
| N9 | Function assay | Inhibitory activity against TNF-alpha release in N9 cells in the supernatant, IC50 = 0.074 μM. | 12361395 | ||
| PBMC | Function assay | Inhibitory concentration against growth of LPS stimulated human peripheral blood mononuclear cells, IC50 = 0.04 μM. | 11229767 | ||
| PBMC | Function assay | Inhibitory concentration against TNF-alpha production from human peripheral blood mononuclear cells stimulated by LPS, IC50 = 0.01 μM. | 11229767 | ||
| T-cell | Function assay | Inhibitory concentration against T cell proliferation using concanavalin A stimulated mice spleen cells, IC50 = 0.005 μM. | 11229767 | ||
| CV1 | Function assay | Agonist activity at human GR expressed in CV1 cells by GRE activation assay, EC50 = 0.0002 μM. | 17705362 | ||
| NHDFneo | Function assay | Activity at human GR expressed in NHDFneo cells assessed as inhibition of IL-6 production, IC50 = 0.0014 μM. | 17705362 | ||
| J774A.1 | Function assay | Inhibition of LPS-induced TNFalpha production in mouse J774A.1 cells, IC50 = 0.048 μM. | 17892941 | ||
| CV1 | Function assay | Activity at human glucocorticoid receptor expressed in CV1 cells assessed as repression of TNF and IL-1-beta-induced E-selectin gene expression by luciferase reporter gene assay, ED50 = 0.0001 μM. | 18032610 | ||
| A549 | Function assay | Agonist activity at glucocorticoid receptor in human A549 cells by MMTV transactivation assay, EC50 = 0.005012 μM. | 18038970 | ||
| A549 | Function assay | Agonist activity at glucocorticoid receptor in human A549 cells by NF-kappaB transrepression assay, IC50 = 0.001175 μM. | 18038970 | ||
| HeLa | Cytotoxicity assay | Cytotoxicity against human HeLa cells assessed as inhibition of DNA replication by imaging analysis | 18066055 | ||
| HeLa | Function assay | Inhibition of mitosis in human HeLa cells by imaging analysis | 18066055 | ||
| THP1 | Antiinflammatory assay | Antiinflammatory activity in human THP1 cells assessed as inhibition of LPS-induced IL6 by ELISA, IC50 = 0.007 μM. | 18625560 | ||
| THP1 | Antiinflammatory assay | Antiinflammatory activity in human THP1 cells assessed as inhibition of LPS-induced TNFalpha by ELISA, IC50 = 0.05 μM. | 18625560 | ||
| RAW264.7 | Function assay | Inhibition of LPS-stimulated microsomal prostaglandin E synthase 1 expression at 10 uM in mouse RAW264.7 cells by Western blot | 18790649 | ||
| A549 | Function assay | Transrepression activity at GR in IL-1-beta-stimulated human A549 cells assessed as inhibition of NF-kappaB-dependent E-selectin transcription by luciferase reporter gene assay, EC50 = 0.0011 μM. | 19321341 | ||
| A549 | Function assay | Transrepression activity at GR in PMA-stimulated human A549 cells assessed as inhibition of AP1 response element-induced luciferase reporter gene activity, EC50 = 0.0025 μM. | 19321341 | ||
| NP1 | Function assay | Agonist activity at GR ligand binding domain expressed in human NP1 cells assessed as glucocorticoid response element transactivation by GAL4 luciferase reporter gene assay, EC50 = 0.0042 μM. | 19321341 | ||
| MDA-kb2 | Function assay | Agonist activity at androgen receptor in human MDA-kb2 cells assessed as stimulation of luciferase activity by luciferase reporter gene assay, EC150 = 0.194 μM. | 19592245 | ||
| MDA-kb2 | Function assay | Agonist activity at glucocorticoid receptor in human MDA-kb2 cells assessed as stimulation of luciferase activity by luciferase reporter gene assay, EC150 = 0.194 μM. | 19592245 | ||
| A549 | Function assay | Agonist activity at GR in human A549 cells by NF-kappaB transrepression assay, IC50 = 0.001 μM. | 19592247 | ||
| COS7 | Function assay | Agonist activity at glucocorticoid receptor ligand binding domain expressed in african green monkey COS7 cells co-transfected with Gal4-LBD by luciferase reporter gene assay, EC50 = 0.0072 μM. | 19863083 | ||
| HeLa | Function assay | Transactivation of GAL-4 tagged glucocorticoid receptor ligand binding domain expressed in human HeLa cells assessed as NP1 activation by luciferase reporter gene assay, EC50 = 0.0045 μM. | 20047280 | ||
| HeLa | Function assay | Transactivation activity at glucocorticoid receptor in human HeLa cells assessed as induction of MMTV promoter activity by luciferase reporter gene assay, EC50 = 0.007943 μM. | 20727743 | ||
| HeLa | Function assay | Transrepression activity at glucocorticoid receptor-mediated antiinflammatory activity in human HeLa cells assessed as inhibition of TPA-induced collagenase promoter activity by luciferase reporter gene assay, IC50 = 0.001585 μM. | 20727743 | ||
| THP1 | Function assay | Transrepression activity at glucocorticoid receptor-mediated antiinflammatory activity in human THP1 cells assessed as inhibition of LPS-induced IL-8 production, IC50 = 0.002512 μM. | 20727743 | ||
| Sf9 | Function assay | Binding affinity to human recombinant glucocorticoid receptor expressed in baculovirus infected Sf9 cells, IC50 = 0.01259 μM. | 20727743 | ||
| insect cells | Function assay | Binding affinity to glucocorticoid receptor expressed in baculovirus-infected insect cells using tetramethylrhodamine labeled Dexamethasone by fluorescence polarization microplate assay, IC50 = 0.0034 μM. | 20735001 | ||
| insect cells | Function assay | Binding affinity to mineralocorticoid receptor expressed in baculovirus-infected insect cells using tetramethylrhodamine labeled Dexamethasone by fluorescence polarization microplate assay, IC50 = 0.033 μM. | 20735001 | ||
| A549 | Function assay | Transrepression activity of glucocorticoid receptor in human A549 cells assessed as inhibition of IL1beta-stimulated NFkappaB-dependent E-selectin transcription by luciferase reporter gene assay, EC50 = 0.0011 μM. | 21073190 | ||
| A549 | Function assay | Transrepression activity of glucocorticoid receptor in human A549 cells expressing AP-1 assessed as inhibition of PMA-induced AP-1 activity by luciferase reporter gene assay, EC50 = 0.0025 μM. | 21073190 | ||
| NP-1 Hela | Function assay | Transactivation activity of glucocorticoid receptor ligand binding domain expressed in human NP-1 Hela cells co-expressing GAL4 DNA binding domain by luciferase reporter gene assay, EC50 = 0.0042 μM. | 21073190 | ||
| A549 | Function assay | Agonist activity at glucocorticoid receptor in human A549 cells by NF-kappaB transrepression assay, IC50 = 0.001 μM. | 21257309 | ||
| A549 | Function assay | Agonist activity at GR in human A549 cells transfected with luciferase gene linked to MMTV promoter assessed as luciferase transactivation activity, IC50 = 0.003981 μM. | 21257309 | ||
| HeLa | Function assay | Agonist activity at glucocorticoid receptor in human HeLa cells transfected with luciferase gene linked to MMTV promoter assessed as luciferase transactivation activity, EC50 = 0.017 μM. | 21963986 | ||
| insect cells | Function assay | Displacement of tetramethylrhodamine-labeled Dexamethasone from human recombinant glucocorticoid receptor expressed in baculovirus infected insect cells by fluorescence polarization assay, IC50 = 0.003 μM. | 21963986 | ||
| insect cells | Function assay | Displacement of tetramethylrhodamine-labeled Dexamethasone from human recombinant mineralocorticoid receptor expressed in baculovirus infected insect cells by fluorescence polarization assay, IC50 = 0.033 μM. | 21963986 | ||
| A549 | Function assay | Transrepression activity at glucocorticoid receptor in human A549 cells assessed as inhibition of IL1beta-stimulated NFkappaB-dependent E-selectin transcription by luciferase reporter gene assay, EC50 = 0.0011 μM. | 23916594 | ||
| A549 | Function assay | Transrepression activity at glucocorticoid receptor in human A549 cells assessed as inhibition of PMA-stimulated AP1 response element by luciferase reporter gene assay, EC50 = 0.0025 μM. | 23916594 | ||
| Hela | Function assay | Transactivation activity at glucocorticoid receptor ligand binding domain (unknown origin) expressed in human Hela cells co-expressing GAL4 DNA binding domain assessed as NP-1-stimulated GRE activation by luciferase reporter gene assay, EC50 = 0.0045 μM. | 23916594 | ||
| A549 | Function assay | Agonist activity at glucocorticoid receptor in human A549 cells assessed as inhibition of IL-1beta-induced NF-kappaB dependent E-selectin activation by luciferase reporter gene assay, EC50 = 0.0011 μM. | 23953070 | ||
| A549 | Function assay | Agonist activity at glucocorticoid receptor in human A549 cells assessed as inhibition of PMA-induced AP-1 activation by luciferase reporter gene assay, EC50 = 0.0025 μM. | 23953070 | ||
| HeLa | Function assay | Transactivation of glucocorticoid receptor ligand binding domain (unknown origin) transfected in human HeLa cells assessed as activation of NP-1 by GAL4 luciferase reporter gene assay, EC50 = 0.0045 μM. | 23953070 | ||
| A549 | Function assay | Transrepression of glucocorticoid receptor in human A549 cells assessed as inhibition of PMA-induced AP-1 activity by luciferase reporter gene assay, EC50 = 0.0025 μM. | 24011644 | ||
| HeLa | Function assay | Transactivation of GR-LBD expressed in human HeLa cells co-expressing GAL4-DBD by luciferase reporter gene assay, EC50 = 0.0042 μM. | 24011644 | ||
| HEK293 | Function assay | Displacement of [3H]-aldosterone from human mineralocorticoid receptor expressed in HEK293 cells, Ki = 0.00036 μM. | 24446728 | ||
| HEK293 | Function assay | Displacement of [3H]-dexamethasone from human glucocorticoid receptor expressed in HEK293 cells, Ki = 0.00069 μM. | 24446728 | ||
| HEK293 | Function assay | Displacement of [3H]-methyltrienolone from human progesterone receptor expressed in HEK293 cells, Ki = 0.561 μM. | 24446728 | ||
| HEK293 | Function assay | Displacement of [3H]-methyltrienolone from human androgen receptor expressed in HEK293 cells, Ki = 1.41 μM. | 24446728 | ||
| HeLa | Function assay | Transactivation of glucocorticoid receptor in human HeLa cells harboring MMTV promoter by luciferase reporter gene assay, EC50 = 0.017 μM. | 24656565 | ||
| A549 | Function assay | Agonist activity at glucocorticoid receptor in human A549 cells assessed as E-selectin transrepression by luciferase reporter gene assay, EC50 = 0.0011 μM. | 24980053 | ||
| A549 | Function assay | Agonist activity at glucocorticoid receptor in human A549 cells assessed as AP-1 transrepression by luciferase reporter gene assay, EC50 = 0.0025 μM. | 24980053 | ||
| HeLa | Function assay | Agonist activity at glucocorticoid receptor in human HeLa cells assessed as NP-1 transactivation by luciferase reporter gene assay, EC50 = 0.0045 μM. | 24980053 | ||
| HEK293 | Function assay | Agonist activity at human GCR expressed in HEK293 cells by luciferase reporter gene assay, EC50 = 0.0013 μM. | 25305688 | ||
| HFF | Function assay | Agonist activity at GR in HFF cells assessed as suppression of IL-1-induced IL-6 production, IC50 = 0.001 μM. | 25516791 | ||
| IM9 | Function assay | Displacement of [3H]dexamethasone from glucocorticoid receptor in human IM9 cells, IC50 = 0.0038 μM. | 26988801 | ||
| IM9 | Function assay | Displacement of [3H]dexamethasone from GR receptor in human IM9 cells, IC50 = 0.0038 μM. | 27876250 | ||
| HeLa | Function assay | Transrepression activity at glucocorticoid receptorin human HeLa cells assessed as inhibition of TPA-induced collagenase promoter activity by luciferase reporter gene assay, IC50 = 0.001585 μM. | 28043796 | ||
| THP1 | Function assay | Transrepression activity at glucocorticoid receptor in human THP1 cells assessed as receptor-mediated anti-inflammatory activity by measuring inhibition of LPS-induced IL-8 production, IC50 = 0.002512 μM. | 28043796 | ||
| HeLa | Function assay | Transactivation activity at glucocorticoid receptor in human HeLa cells assessed as induction of MMTV promoter activity by luciferase reporter gene assay, IC50 = 0.007943 μM. | 28043796 | ||
| Sf9 | Function assay | Binding affinity to recombinant human glucocorticoid receptor expressed in baculovirus infected sf9 cells, IC50 = 0.01259 μM. | 28043796 | ||
| RAW264.7 | Antiinflammatory assay | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production by griess assay, IC50 = 0.8 μM. | 29272126 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 29435139 | ||
| BV2 | Antiinflammatory assay | Antiinflammatory activity in mouse BV2 cells assessed as inhibition of LPS-induced nitric oxide production, IC50 = 9.5 μM. | 29482940 | ||
| RAW264.7 | Antiinflammatory assay | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production, IC50 = 8.3 μM. | 29741372 | ||
| HEK 293T | Function assay | Agonist activity at GAL4 DNA-binding domain fused GR (unknown origin) ligand binding domain expressed in UAS-bla HEK 293T cells assessed as beta-lactamase transcriptional activation by FRET-based GeneBLAzer assay, IC50 = 0.00235 μM. | 30144697 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Dexamethasone是一种有效的半合成的糖皮质激素类甾体药物，也是一种interleukin receptor调节剂，具有抗炎和免疫抑制作用。Dexamethasone 可诱导自噬和线粒体自噬。Dexamethasone 被用于COVID-19临床病人测试中，并发现对危重症患者有一定效果。 | |
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| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | 在永生化鼠脑内皮细胞株（GPNT）中，Dexamethasone导致了单层细胞对蔗糖，荧光素和20 KDa葡聚糖通透性的降低。在培养的大鼠脑血管内皮细胞的细胞质中，Dexamethasone导致丝状肌动蛋白和相关的细胞骨架蛋白皮层蛋白被高度集中在很少的F-肌动蛋白应力纤维可见的细胞和细胞接触的区域，这和Dexamethasone诱导的分化障碍表型一致。Dexamethasone强烈刺激的Id-1蛋白的表达，它是血清诱导的螺旋-环-螺旋转录抑制子，参与细胞分化的水平，并且这种作用被证明是在CON8乳腺上皮肿瘤细胞的细胞周与ZO-1的重组相关联。Dexamethasone可防止细胞因子诱导MMP-9表达的增强，并在未处理GPNT单层细胞中抑制ZO-1表达。 [1] 在肺泡上皮细胞中，Dexamethasone通过下调伽玛GCS重亚单位的转录消耗基础和肿瘤坏死因子-α刺激的谷胱甘肽水平下调，通过AP-1（c-Jun）途径。在肺泡上皮细胞（A549）中，Dexamethasone降低基础和刺激的GSH水平（TNF-α处理的），而不对GSSG有任何变化。[3] |
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| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | Bcl-2 / Bcl-xl / Mcl-1 / Survivin / IAP1 Cyclin D1 / Cyclin E / COX-2 / MMP-9 Bax / p21 p-JNK / JNK / p-p38 / p38 / p-ERK / ERK |
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28696369 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | 在肺泡上皮细胞中，Dexamethasone肌肉注射给药到怀孕母羊，导致了以下结果（1）血压不变; （2）如先前在胎儿报道，感光度为内皮素-1（ET）的增加; （3）乙酰胆碱诱导的舒张是增加的; （4）L-NAME对ET可抑制血管舒张反应被废除; （5）存在于内皮依赖性血管舒张功能没有变化;（6）相比于盐水治疗的对照组，eNOS的RNA和蛋白水平没有变化。 [3] |
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|---|---|---|
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT06351644 | Not yet recruiting | Relapsed and/or Refractory Multiple Myeloma |
Adriana Rossi|Icahn School of Medicine at Mount Sinai |
June 3 2024 | Phase 1|Phase 2 |
| NCT06367855 | Not yet recruiting | Spinal Stenosis Lumbar|Disc Degeneration|Disc Disease|Fusion of Spine|Surgery |
Potsawat Surabotsopon|Thammasat University Hospital |
May 1 2024 | Phase 4 |
| NCT06367725 | Recruiting | Acute Lymphoblastic Leukemia |
University of Aarhus |
April 11 2024 | -- |
化学信息&溶解度
| 分子量 | 392.46 | 分子式 | C22H29FO5 |
| CAS号 | 50-02-2 | SDF | Download Dexamethasone SDF |
| Smiles | CC1CC2C3CCC4=CC(=O)C=CC4(C3(C(CC2(C1(C(=O)CO)O)C)O)F)C | ||
| 储存条件(自收到货起) | powder, 4°C (in the dark) ; in solvent，-80°C (in the dark) | ||
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体外溶解度 |
DMSO : 200 mg/mL ( (509.6 mM) Ultrasonicated; ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Ethanol : 20 mg/mL (50.96 mM) Water : Insoluble |
摩尔浓度计算器 |
|
体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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常见问题及建议解决方法
问题 1:
I'm loonkig for Dexamethasone to use in cell culture, would it be better to use the Dexamethasone S1322, the sodiume phosphate S4028 or the acetate S3124?
回答：
S1322 is the free base form of Dexamethasone, S4028 is the sodium phosphate form and S3124 is the acetate salt. All of them have similar biological activity in tissue culture, however, their suitabilities vary in different solvents. As free base, S1322 has high solubility in DMSO (79mg/ml), poor solubility in water (<1mg/ml), and moderate solubility in ethanol (6mg/ml). As sodium phosphate salt, S4028 has high solubility in water (103mg/ml) but is insoluble in DMSO and ethanol (<1mg/ml). The solubility of S3124 is 87mg/ml in DMSO, <1mg/ml in water, and 20mg/ml in ethanol. Selection can be made based on the customer's experimental setup.
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