Rosiglitazone
别名: BRL 49653 中文名称：罗格列酮
Rosiglitazone是有效的降糖药，也是有效的噻唑烷二酮类胰岛素增敏剂，在大鼠，3T3-L1和人体脂肪细胞中IC50分别为12，4和9 nM。Rosiglitazone是PPAR-gamma的配体，对PPAR-alpha没有结合力。Rosiglitazone 可调控 TRP channels 并诱导自噬。Rosiglitazone可阻止铁死亡。
Rosiglitazone Chemical Structure
CAS: 122320-73-4
产品质控
批次：
纯度：
99.99%
99.99
Rosiglitazone相关产品
相关信号通路图
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 |
|---|---|---|---|---|---|
| MCF7 | Function assay | 0.1 uM | 24 hrs | Activation of human PPAR-gamma-dependent transcription expressed in human MCF7 cells assessed as induction of PPRE-reporter gene expression at 0.1 uM after 24 hrs by dual luciferase reporter gene assay relative to rosiglitazone | 19719236 |
| HEK293T | Function assay | 1 uM | 24 hrs | Partial agonist activity at human PPARgamma-LBD expressed in HEK293T cells assessed as induction of receptor transactivation at 1 uM after 24 hrs by luciferase reporter gene assay | 21030263 |
| HepG2 | Function assay | 10 umol/L | 24 hrs | Increase in glucose consumption in human HepG2 cells at 10 umol/L after 24 hrs relative to control | 21256748 |
| Ac2F | Function assay | 0.1 to 10 uM | 6 hrs | Agonist activity at PPARgamma in rat Ac2F cells assessed as luciferase activity at 0.1 to 10 uM after 6 hrs by reporter gene assay | 22819190 |
| THP1 | Function assay | 100 uM | 3 hrs | Transactivation of PPARgamma in human THP1 cells assessed as decrease in LPS-induced MCP1 mRNA expression at 100 uM preincubated for 3 hrs prior to LPS challenge measured after 18 hrs by RT-PCR analysis relative to untreated control | 22934537 |
| THP1 | Function assay | 100 uM | 3 hrs | Transactivation of PPARgamma in human THP1 cells assessed as decrease in LPS-induced IL6 mRNA expression at 100 uM preincubated for 3 hrs prior to LPS challenge measured after 18 hrs by RT-PCR analysis relative to untreated control | 22934537 |
| HepG2 | Function assay | 10 uM | 24 hrs | Reduction of glucose consumption in insulin-resistant human HepG2 cells at 10 uM after 24 hrs by glucose oxidase method in presence of 0.1 uM of insulin | 23025244 |
| HepG2 | Function assay | 10 uM | 24 hrs | Reduction of glucose consumption in insulin-resistant human HepG2 cells at 10 uM after 24 hrs by glucose oxidase method in presence of 22.2 mM of glucose | 23025244 |
| CMT93 | Function assay | 10 uM | 30 mins | Induction of PPAR-gamma promoter activity in LPS-stimulated mouse CMT93 cells at 10 uM preincubated for 30 mins before LPS-challenge measured after 6 hrs post challenge by luciferase reporter gene assay | 23416190 |
| HEK293 | Function assay | 10 uM | 24 hrs | Transactivation of PPAR-gamma (unknown origin) expressed in HEK293 cells at 10 uM after 24 hrs by luciferase reporter gene assay | 24890090 |
| HepaR | Function assay | 1 uM | 1 day | Agonist activity at PPARgamma in human HepaR cells assessed as increase in FABP1 gene expression at 1 uM incubated for 1 day by quantitative PCR method relative to untreated control | 25497132 |
| HepaR | Function assay | 1 uM | 1 day | Agonist activity at PPARgamma in human HepaR cells assessed as increase in ANGPTL4 gene expression at 1 uM incubated for 1 day by quantitative PCR method relative to untreated control | 25497132 |
| HepaR | Function assay | 1 uM | 1 day | Agonist activity at PPARgamma in human HepaR cells assessed as increase in HMGCS2 gene expression at 1 uM incubated for 1 day by quantitative PCR method relative to untreated control | 25497132 |
| C2C12 | Function assay | 30 uM | 2 hrs | Induction of 2-deoxy-[3H]-glucose uptake in mouse C2C12 cells at 30 uM after 2 hrs by liquid scintillation counting analysis | 25835537 |
| HEK293 | Function assay | 10 uM | 24 hrs | Agonist activity at PPARgamma (unknown origin) expressed in HEK293 cells assessed as receptor transactivation at 10 uM incubated for 24 hrs by luciferase reporter gene assay | 26384286 |
| HEK293 | Function assay | 1 uM | 24 hrs | Agonist activity at PPAR gamma (unknown origin) transfected in HEK293 cells at 1 uM after 24 hrs by dual-luciferase reporter gene assay | 26988304 |
| C2C12 | Function assay | 20 uM | 4 hrs | Transactivation of PPARgamma in mouse C2C12 cells assessed as increase in GLUT-4 mediated 2-NBDG uptake at 20 uM at 4 hrs by fluorescence assay | 27100993 |
| HT-29 | Function assay | 10 uM | 24 hrs | Agonist activity at PPARgamma in human HT-29 cells harboring APC mutant assessed as inhibition of Wnt/beta-catenin signaling pathway by measuring decrease in CyclinD1 level at 10 uM treated for 24 hrs by Western blot method | 28076827 |
| Ac2F | Function assay | 5 uM | 6 hrs | Agonist activity at full length human flag-tagged PPARgamma1 LBD expressed in rat Ac2F cells coexpressing PPRE-X3-TK at 5 uM after 6 hrs by one-glo luciferase reporter gene assay | 29389121 |
| 3T3-L1 | Function assay | 1 uM | 15 days | Agonist activity at PPARgamma in mouse 3T3-L1 cells assessed as increase in CD36 mRNA expression at 1 uM after 15 days by quantitative real-time PCR method | 29878767 |
| 3T3-L1 | Function assay | 1 uM | 15 days | Agonist activity at PPARgamma in mouse 3T3-L1 cells assessed as induction of adipocyte differentiation at 1 uM after 15 days by Oil Red O staining-based assay | 29878767 |
| 3T3-L1 | Function assay | 1 uM | 15 days | Agonist activity at PPARgamma in mouse 3T3-L1 cells assessed as increase in CPT1A mRNA expression at 1 uM after 15 days by quantitative real-time PCR method | 29878767 |
| HepG2 | Function assay | >100 nM | 20 hrs | Transactivation of GAL4-tagged human PPARgamma LBD expressed in human HepG2 cells at >100 nM after 20 hrs in presence of 5 uM PPARgamma antagonist GW9662 by luciferase reporter gene assay | 30199253 |
| 3T3L1 | Function assay | 10 uM | 24 hrs | Induction of insulin-stimulated 2-deoxy-D-[3H]-glucose uptake in differentiated mouse 3T3L1 cells at 10 uM after 24 hrs by scintillation counting analysis | ChEMBL |
| 3T3L1 | Function assay | 2 uM | 14 days | Agonist activity at PPAR in mouse 3T3L1 cells assessed as increase in adipocyte differentiation at 2 uM after 14 days by Oil Red O staining method | ChEMBL |
| U2OS | Function assay | 10 uM | 24 hrs | Activation of PPARG (unknown origin) expressed in human U2OS cells at 10 uM incubated for 24 hrs by luciferase reporter gene assay | ChEMBL |
| 3T3L1 | Function assay | 10 uM | Increase in adiponectin mRNA levels in TNFalpha-induced mouse 3T3L1 cells pretreated at 10 uM before TNF-alpha challenge relative to control | 21851089 | |
| HEK293 | Function assay | 10 uM | Transactivation of PPARgamma (unknown origin) expressed in HEK293 cells co-transfected with AP2-PPRE at 10 uM by luciferase reporter gene assay | 23273519 | |
| 3T3L1 | Function assay | 2 uM | Transactivation of PPARgamma in mouse 3T3L1 cells assessed as adipocyte differentiation by measuring lipid accumulation at 2 uM by Oil Red O staining-based assay | 26595749 | |
| 3T3L1 | Function assay | 2 uM | Transactivation of PPARgamma in mouse 3T3L1 cells assessed as increase in FABP4 expression at 2 uM by qPCR method | 26595749 | |
| 3T3L1 | Function assay | 2 uM | Transactivation of PPARgamma in mouse 3T3L1 cells assessed as increase in GTUT4 expression at 2 uM by qPCR method | 26595749 | |
| 3T3L1 | Function assay | 2 uM | Transactivation of PPARgamma in mouse 3T3L1 cells assessed as increase in adiponectin expression at 2 uM by qPCR method | 26595749 | |
| 3T3L1 | Function assay | 2 uM | Transactivation of PPARgamma in mouse 3T3L1 cells assessed as increase in LPL expression at 2 uM by qPCR method | 26595749 | |
| 3T3L1 | Function assay | 5 uM | Induction of lipid accumulation in mouse 3T3L1 cells at 5 uM by Oil Red O staining-based assay | 30199253 | |
| 3T3L1 | Function assay | 2 uM | Induction of lipid accumulation in mouse 3T3L1 cells at 2 uM by Oil Red O staining-based assay | 30199253 | |
| CV1 | Function assay | 24 hrs | Agonist activity at human PPARgamma in CV1 cells by GAL4 transactivation assay after 24 hrs, EC50 = 0.03 μM. | 17507225 | |
| CV1 | Function assay | 24 hrs | Agonist activity at human PPARalpha in CV1 cells by GAL4 transactivation assay after 24 hrs, EC50 = 3.46 μM. | 17507225 | |
| COS1 | Function assay | 48 hrs | Agonist activity at human recombinant PPARgamma expressed in COS1 cells co-expressing GAL4 assessed as transcriptional activity after 48 hrs by luciferase reporter gene assay, EC50 = 0.02 μM. | 19507861 | |
| 3T3L1 | Function assay | 7 days | Induction of adipogenesis in mouse 3T3L1 cells assessed as increase in lipid accumulation after 7 days by Oil red O staining | 20527969 | |
| HEK293 | Function assay | 16 to 20 hrs | Transactivation of Gal4-fused human PPARgamma expressed in HEK293 cells after 16 to 20 hrs by luciferase reporter gene assay, EC50 = 0.043 μM. | 21128600 | |
| CV1 | Function assay | 40 hrs | Agonist activity at human PPARgamma-LBD expressed in CV1 cells co-transfected with Gal4 after 40 hrs by luciferase based transactivation assay, EC50 = 0.1 μM. | 21515063 | |
| COS-1 | Function assay | 24 hrs | Agonist activity at human PPARgamma ligand binding domain expressed in COS-1 cells after 24 hrs by luciferase reporter gene-based luminometric analysis, EC50 = 0.048 μM. | 22051054 | |
| HepG2 | Function assay | 20 hrs | Agonist activity at human GAL4-fused PPARgamma ligand binding domain expressed in HepG2 cells after 20 hrs by luciferase reporter gene transactivation assay, EC50 = 0.02 μM. | 22081932 | |
| COS1 | Function assay | 24 hrs | Transactivation of human full length PPARgamma expressed in COS1 cells co-transfected with RXRalpha after 24 hrs by luciferase reporter gene assay, EC50 = 0.12 μM. | 22197396 | |
| 293H DA | Function assay | 16 hrs | Agonist activity at PPARgamma LBD in human 293H DA cells after 16 hrs by TR-FRET activation reporter assay, EC50 = 0.0024 μM. | 22582973 | |
| MG-63 | Function assay | 24 hrs | Modulation of full-length human pSG5-fused PPARgamma expressed in MG-63 cells co-expressing pGV-P2-PPRE after 24 hrs by luciferase reporter gene based transactivation assay, EC50 = 0.011 μM. | 22727448 | |
| HepG2 | Function assay | 20 hrs | Transactivation of GAL4-fused human PPARgamma ligand binding domain expressed in HepG2 cells after 20 hrs by luciferase reporter gene assay, EC50 = 0.039 μM. | 23171045 | |
| L02 | Function assay | 24 hrs | Agonist activity at PPARgamma-LBD expressed in human L02 cells co-expressing pGL3-SV40-GAL4 after 24 hrs by luciferase reporter gene based transactivation assay, EC50 = 0.9 μM. | 23186307 | |
| HEK293 | Function assay | 48 hrs | Agonist activity at human PPARgamma expressed in HEK293 cells cotransfected with PPREx4-TK-luc assessed as activation of luciferase activity measured after 48 hrs by transactivation assay, EC50 = 43.71 μM. | 23265844 | |
| HEK293 | Function assay | 24 hrs | Transactivation of GAL4 DBD-fused human PPARgamma-LBD expressed in HEK293 cells after 24 hrs by luciferase reporter gene assay, EC50 = 0.1 μM. | 23294830 | |
| L6 | Function assay | 24 hrs | Induction of glucose uptake in rat L6 cells pulsed with C14-deoxy glucose after 24 hrs in presence of insulin, EC50 = 4.49 μM. | 23992862 | |
| L6 | Function assay | 16 hrs | Increase in 2-[3H]-deoxyglucose uptake in rat L6 cells after 16 hrs by scintillation counting analysis, IC50 = 4.8 μM. | 24813738 | |
| HEK293 | Function assay | 24 hrs | Agonist activity at mouse PPARgamma expressed in HEK293 cells co-expressing with Gal4 reporter vector after 24 hrs by dual-luciferase reporter assay, EC50 = 0.03 μM. | 24955889 | |
| DU145 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human DU145 cells assessed as growth inhibition after 48 hrs by MTT assay, IC50 = 16 μM. | 24996143 | |
| PC3 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human PC3 cells assessed as growth inhibition after 48 hrs by MTT assay, IC50 = 20.3 μM. | 24996143 | |
| MDA-MB-231 | Growth inhibition assay | 24 hrs | Growth inhibition of human MDA-MB-231 cells after 24 hrs by MTT assay, IC50 = 5.23 μM. | 25278236 | |
| HepG2 | Function assay | 20 hrs | Transactivation of PPAR transfected in human HepG2 cells after 20 hrs by PPAR-luciferase assay, EC50 = 1.6 μM. | 25437304 | |
| HEK293 | Function assay | 24 hrs | Transactivation of PPARgamma (unknown origin) expressed in HEK293 cells incubated for 24 hrs by luciferase reporter gene assay | 25442322 | |
| HepG2 | Function assay | 20 hrs | Agonist activity at GAL4-DNA binding domain fused human PPARgamma ligand binding domain expressed in human HepG2 cells assessed as receptor transactivation incubated for 20 hrs by luciferase reporter gene assay, EC50 = 0.04 μM. | 25497132 | |
| MCF7 | Function assay | 16 hrs | Agonist activity at human PPARgamma transfected in human MCF7 cells after 16 hrs by luciferase reporter gene assay, EC50 = 0.087 μM. | 26226490 | |
| HEK293 | Function assay | 24 hrs | Agonist activity at GAL4-tagged human PPARgamma ligand binding domain chimeric receptor expressed in HEK293 cells after 24 hrs by luciferase reporter gene assay, EC50 = 0.26 μM. | 27591006 | |
| HepG2 | Function assay | 20 hrs | Transactivation of GAL4-fused human PPARgamma LBD expressed in human HepG2 cells after 20 hrs by luciferase reporter gene assay, EC50 = 0.04 μM. | 28076827 | |
| COS7 | Function assay | 24 hrs | Transactivation of human Gal4-fused PPARgamma LBD expressed in African green monkey COS7 cells after 24 hrs by luciferase reporter gene assay, EC50 = 0.004 μM. | 28609708 | |
| COS7 | Function assay | 24 hrs | Transactivation of human Gal4-fused PPARalpha LBD expressed in African green monkey COS7 cells after 24 hrs by luciferase reporter gene assay, EC50 = 10 μM. | 28609708 | |
| HEK293 | Function assay | 18 hrs | Agonist activity at GAL4-fused PPARgamma LBD (unknown origin) expressed in HEK293 cells assessed as receptor transactivation after 18 hrs by dual luciferase reporter gene assay, EC50 = 0.04 μM. | 28667876 | |
| HepG2 | Function assay | 20 hrs | Transactivation of GAL4-tagged human PPARgamma LBD expressed in human HepG2 cells after 20 hrs by luciferase reporter gene assay, EC50 = 0.039 μM. | 30199253 | |
| COS7 | Function assay | 24 hrs | Agonist activity at recombinant human GAL4-DBD fused PPARgamma LBD expressed in COS7 cells after 24 hrs by luciferase reporter gene assay, EC50 = 0.396 μM. | 30220602 | |
| COS7 | Function assay | 24 hrs | Agonist activity at recombinant human GAL4-DBD fused PPARgamma LBD expressed in COS7 cells after 24 hrs by luciferase reporter gene assay, EC50 = 0.396 μM. | 30241907 | |
| HEK293 | Function assay | 18 hrs | Agonist activity at human GAL4 fused PPARgamma-LBD expressed in HEK293 cells after 18 hrs by luciferase reporter gene assay, EC50 = 0.12 μM. | 30296685 | |
| HEL 293H | Function assay | 16 hrs | Transactivation of GAL4-DBD fused human PPARgamma ligand binding domain expressed in UAS-bla HEL 293H cells preincubated for 16 hrs followed by FRET substrate addition and measured after 2 hrs by TR-FRET assay, EC50 = 0.008 μM. | 30429097 | |
| HEK293 | Function assay | 18 hrs | Transactivation of human PPARgamma expressed in HEK293 cells incubated for 18 hrs by dual luciferase reporter gene assay, EC50 = 0.039 μM. | ChEMBL | |
| 3T3L1 | Function assay | 7 days | Upregulation of FAS protein expression in differentiated mouse 3T3L1 cells after 7 days by western blot analysis | ChEMBL | |
| 3T3L1 | Function assay | 7 days | Upregulation of aP2 protein expression in differentiated mouse 3T3L1 cells after 7 days by western blot analysis | ChEMBL | |
| 3T3L1 | Function assay | 24 hrs | Inhibition of chronic insulin-stimulated insulin resistance in differentiated mouse 3T3L1 cells assessed as 2-deoxy-D-[3H]-glucose uptake after 24 hrs by scintillation counting analysis | ChEMBL | |
| COS1 | Function assay | In vitro agonist activity tested for transactivation in human PPAR gamma-Gal4 chimeric COS-1 cells, EC50 = 0.02 μM. | 12729668 | ||
| COS1 | Function assay | Agonistic activity was determined in COS1 cells transfected with GAL 4-PPAR gamma receptor, EC50 = 0.021 μM. | 12617924 | ||
| CV-1 | Function assay | Maximal reporter activity against human Peroxisome proliferator activated receptor gamma Gal4 chimeric in transiently transfected CV-1 cells by functional assay., EC50 = 0.043 μM. | 11720854 | ||
| 3T3-L1 | Function assay | Stimulation of adipogenesis in 3T3-L1 cells is expressed as concentration equivalent to the [ 1-14C] uptake counts after treatment with 0.2 ug/mL troglitazone, EC = 0.09 μM. | 10956213 | ||
| CV-1 | Function assay | Activation of peroxisome proliferator activated receptor gamma measured by induction of 50% of maximum alkaline phosphatase activity, transfection assay in CV-1 cells, EC50 = 0.08913 μM. | 9836620 | ||
| CV-1 | Function assay | In vitro transcriptional activation of Peroxisome proliferator activated receptor gamma (PPAR) expressed in CV-1 cells, EC50 = 0.06 μM. | 8576907 | ||
| HepG2 | Function assay | Effective concentration against human PPARgamma expressed in HepG2 cells, EC50=0.02 μM | 15801817 | ||
| COS1 | Function assay | In vitro transactivation of human peroxisome proliferator activated receptor gamma measured in PPAR-GAL4 chimeric COS-1 cells, EC50 = 0.02 μM. | 12873517 | ||
| CV-1 | Function assay | In vitro evaluation against RXR-alpha/PPAR-gamma in CV-1 cells by cotransfection assay was determined, EC50 = 0.325 μM. | 12954061 | ||
| 3T3-L1 | Function assay | Effective concentration for enhancement of insulin-induced triglyceride accumulation in 3T3-L1 cells, EC30 = 0.02 μM. | 14505644 | ||
| HepG2 | Function assay | Effective concentration against human PPARgamma expressed in HepG2 cells, EC50 = 0.039 μM. | 16107150 | ||
| U2OS | Function assay | Effect on PPARgamma transactivation activity in U2OS cells, EC50 = 0.03 μM. | 16300944 | ||
| Huh7 | Function assay | Functional activity at human PPAR gamma in Huh7 cells by transactivation assay, EC50 = 0.22 μM. | 16366601 | ||
| Huh7 | Function assay | Effect on PPAR gamma transactivation activity in Huh7 cells, EC50 = 0.22 μM. | 16451087 | ||
| HEK293 | Function assay | Agonist activity at PPARgamma expressed in HEK293 cells assessed as induction of receptor interaction with steroid receptor coactivator-1 by EYFP based reporter gene assay | 16680159 | ||
| HEK293 | Function assay | Agonist activity at PPARgamma expressed in HEK293 cells assessed as induction of receptor interaction with retinoid X-receptor alpha by EYFP based reporter gene assay | 16680159 | ||
| CV1 | Function assay | Transactivation of PPARgamma in CV1 cells, EC50 = 0.076 μM. | 16821769 | ||
| NIH3T3 | Function assay | Activity at human PPAR gamma transfected in NIH3T3 cells by luciferase activity assay, EC50 = 0.32 μM. | 16854085 | ||
| CV1 | Function assay | Transactivation of human PPARgamma in CV1 cells by luciferase reporter gene assay, EC50 = 0.308 μM. | 16970391 | ||
| HepG2 | Function assay | Agonist activity at human PPAR gamma in a HepG2 cells by PPAR-GAL4 transactivation assay, EC50 = 0.158 μM. | 16973358 | ||
| HepG2 | Function assay | Agonist activity at human PPAR gamma in HepG2 cells by PPAR-GAL4 transactivation assay, EC50 = 0.158 μM. | 16979341 | ||
| CV1 | Function assay | Activity at human PPARgamma in CV1 cells, EC50 = 0.308 μM. | 17005394 | ||
| Huh7 | Function assay | Activity at human PPAR gamma in Huh7 cells by transactivation assay, EC50 = 0.22 μM. | 17034149 | ||
| CV1 | Function assay | Agonist activity at PPARgamma in CV1 cells by transactivation assay, EC50 = 0.308 μM. | 17129725 | ||
| HepG2 | Function assay | Agonist activity at human PPARgamma in HepG2 cells by PPAR-GAL4 transactivation assay, EC50 = 0.082 μM. | 17157019 | ||
| HEK293 | Function assay | Agonist activity at PPARgamma receptor expressed in HEK293 cells by GAL4 transactivation assay, EC50 = 0.035 μM. | 17292606 | ||
| HEK293 | Function assay | Activity at human adipose tissue PPAR gamma expressed in HEK293 cells by PPAR-GAL4 transactivation assay, EC50 = 0.31 μM. | 17343371 | ||
| L6 | Function assay | Effect on fatty acid oxidation in rat L6 cells, EC50 = 5 μM. | 17343371 | ||
| HepG2/C3A | Function assay | Activation of human PPARgamma ligand binding domain-mediated transcriptional activity in human HepG2/C3A cells co-transfected with fused Gal4-LBD by cotransfection assay, EC50 = 0.0038 μM. | 17403688 | ||
| NIH3T3 | Function assay | Agonist activity at human PPARgamma expressed in NIH3T3 cells by GAL4 transactivation assay, EC50 = 0.32 μM. | 17624777 | ||
| HEK293 | Function assay | Agonist activity at PPARgamma expressed in HEK293 cells assessed as aP2 gene induction, EC50 = 0.12 μM. | 18029176 | ||
| HEK293 | Function assay | Agonist activity at PPARgamma expressed in HEK293 cells by GAL4 transactivation assay, EC50 = 0.19 μM. | 18029176 | ||
| CV1 | Function assay | Agonist activity at human PPARgamma expressed in CV1 cells by receptor transactivation assay, EC50 = 0.308 μM. | 18029178 | ||
| HEK293 | Function assay | Agonist activity at PPARgamma in HEK293 cells by GAL4 transactivation assay, EC50 = 0.045 μM. | 18291645 | ||
| U2OS | Function assay | Agonist activity at human PPARgamma in U2OS cells by transactivation assay, EC50 = 0.02 μM. | 18329751 | ||
| HepG2 | Function assay | Agonist activity at human PPARgamma expressed in HepG2 cells by GAL4 transactivation assay, EC50 = 0.223 μM. | 18394907 | ||
| HepG2 | Function assay | Agonist activity at PPARgamma expressed in human HepG2 cells assessed as induction of receptor transactivation by reporter gene assay relative to control, EC50 = 0.05 μM. | 18625559 | ||
| RAW264.7 | Function assay | Suppression of LPS/IFN-gamma-stimulated NO production in mouse RAW264.7 cells, IC50 = 17.5 μM. | 18809325 | ||
| CV1 | Function assay | Agonist activity at human PPARgamma ligand binding domain expressed in african green monkey CV1 cells co-transfected with fused Gal4-DBD by transactivation assay, EC50 = 0.033 μM. | 18826205 | ||
| CV1 | Function assay | Agonist activity at human PPARalpha ligand binding domain expressed in african green monkey CV1 cells co-transfected with fused Gal4-DBD by transactivation assay, EC50 = 3.46 μM. | 18826205 | ||
| HepG2 | Function assay | Agonist activity at human PPARalpha ligand binding domain expressed in human HepG2 cells co-transfected with Gal4 by luciferase reporter gene assay, EC50 = 0.039 μM. | 18835719 | ||
| HepG2 | Function assay | Agonist activity at human PPARgamma ligand binding domain expressed in human Hep G2 cells co-transfected with Gal4-DBD by luciferase reporter gene assay, EC50 = 0.04 μM. | 19053776 | ||
| HeLa | Function assay | Agonist activity at PPARgamma ligand binding domain expressed in human HeLa cells co-transfected with Gal4-DBD assessed as transcriptional activation by Gal4 response element-driven luciferase reporter gene assay, EC50 = 0.015 μM. | 19275963 | ||
| BL21 | Function assay | Displacement of radio labeled 2(S)-(2-benzoyl-phenylamino)-3-{4-[1,1-ditritio-2-(5-methyl-2-phenyl-oxazol-4-yl)-ethoxy]-phenyl}-propionic acid from GST-fused human PPARgamma expressed in Escherichia coli BL21 cells by scintillation proximity assay, IC50 = 0.45 μM. | 19349176 | ||
| BHK21 | Function assay | Agonist activity at human PPARgamma expressed in BHK21 cells assessed as SEAP activity by luciferase reporter transactivation assay, EC50 = 0.45 μM. | 19349176 | ||
| COS1 | Function assay | Agonist activity at human PPARgamma receptor expressed in african green monkey COS1 cells co-transfected with fused yeast Gal4-DBD by transactivation assay, EC50 = 0.02 μM. | 19530681 | ||
| U2OS | Function assay | Agonist activity at human PPARgamma expressed in U2OS cells by luciferase transactivation assay, EC50 = 0.05 μM. | 19574056 | ||
| HepG2 | Function assay | Agonist activity at GAL4-tagged human PPARgamma ligand binding domain expressed in human HepG2 cells assessed as receptor transactivation by luciferase reporter gene assay, EC50 = 0.039 μM. | 19775169 | ||
| HepG2 | Function assay | Agonist activity at human PPARgamma expressed in HepG2 cells by GAL4 transactivation assay, EC50 = 0.223 μM. | 19783444 | ||
| COS7 | Function assay | Agonist activity at human recombinant PPARgamma1 LBD expressed in african green monkey COS7 cells coexpressing GAL4 by luciferase reporter gene transactivation assay, EC50 = 0.03 μM. | 20138762 | ||
| COS7 | Function assay | Agonist activity at human recombinant PPARgamma2 LBD expressed in african green monkey COS7 cells coexpressing GAL4 by luciferase reporter gene transactivation assay, EC50 = 0.1 μM. | 20138762 | ||
| HEK | Function assay | Agonist activity at human GAL4-tagged PPARgamma chimeric receptor expressed in HEK cells by transactivation assay, EC50 = 0.035 μM. | 20299214 | ||
| HEK | Function assay | Agonist activity at human GAL4-tagged PPARalpha chimeric receptor expressed in HEK cells by transactivation assay, EC50 = 10.58 μM. | 20299214 | ||
| CHO-K1 | Function assay | Partial agonist activity at human PPARgamma-LBD expressed in CHO-K1 cells co-transfected with GAL4 assessed as luciferase activity by transactivation assay, EC50 = 0.1 μM. | 20527969 | ||
| CV1 | Function assay | Transactivation of Gal4-fused human PPARgamma DNA binding domain expressed in african green monkey CV1 cells by luciferase reporter gene assay, EC50 = 0.1 μM. | 21112784 | ||
| HepG2 | Function assay | Transactivation of human PPARgamma expressed in human HepG2 cells co-transfected with PPRE3-TK-Luc by luciferase reporter gene assay, EC50 = 0.05 μM. | 21450468 | ||
| HepG2 | Function assay | Agonist activity at PPARgamma receptor expressed in human HepG2 cells by PPRE-luciferase reporter gene assay, EC50 = 0.01 μM. | 21482446 | ||
| COS7 | Function assay | Modulation of human PPARgamma-LBD expressed in african green monkey COS7 cells co-transfected with Gal4 assessed as activation of transactivation activity by luciferase assay, EC50 = 0.043 μM. | 21873070 | ||
| Sf21 | Function assay | Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake, IC50 = 6.4 μM. | 21965623 | ||
| Sf21 | Function assay | Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake, IC50 = 40 μM. | 21965623 | ||
| COS1 | Function assay | Binding affinity to human wild type PPARgamma LBD expressed in COS1 cells co-expressing GAL4 by scintillation proximity assay | 22070604 | ||
| BL21 DE3 | Function assay | Displacement of [3H]rosiglitazone from N-terminal His-tagged human PPARgamma ligand binding domain expressed in Escherichia coli BL21 DE3 cells by scintillation proximity assay, Ki = 0.074 μM. | 22081932 | ||
| MG-63 | Function assay | Agonist activity at human PPARgamma expressed in MG-63 cells by reporter gene-based transactivation assay, EC50 = 0.011 μM. | 22225641 | ||
| HepG2 | Function assay | Transactivation of GAL4-fused PPARgamma ligand binding domain transfected in human HepG2 cells by luciferase reporter gene assay, EC50 = 0.1 μM. | 22934537 | ||
| HEK293 | Function assay | Agonist at human PPARgamma LBD expressed in human HEK293 cells cotransfected with GAL4-Luc assessed as transcriptional activation by luciferase reporter gene assay, EC50 = 0.004 μM. | 23286787 | ||
| HepG2 | Function assay | Agonist activity at GAL4-fused PPARgamma M463A mutant (unknown origin) expressed in human HepG2 cells by transactivation assay, EC50 = 0.002 μM. | 23502212 | ||
| HepG2 | Function assay | Agonist activity at GAL4-fused PPARgamma (unknown origin) expressed in human HepG2 cells by transactivation assay, EC50 = 0.01 μM. | 23502212 | ||
| HEK293 | Function assay | Agonist activity at human PPARgamma expressed in HEK293 cells by luciferase reporter gene assay, EC50 = 0.01 μM. | 25305688 | ||
| HepG2 | Function assay | Agonist activity at human GAL4-PPARgamma ligand binding domain expressed in human HepG2 cells by luciferase reporter gene assay, EC50 = 0.039 μM. | 25462281 | ||
| 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 | ||
| CV-1 | Function assay | Tested for transactivation of human PPAR gamma-Gal4 chimera in CV-1 cells, EC50 = 0.05 μM. | ChEMBL | ||
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生物活性
| 产品描述 | Rosiglitazone是有效的降糖药，也是有效的噻唑烷二酮类胰岛素增敏剂，在大鼠，3T3-L1和人体脂肪细胞中IC50分别为12，4和9 nM。Rosiglitazone是PPAR-gamma的配体，对PPAR-alpha没有结合力。Rosiglitazone 可调控 TRP channels 并诱导自噬。Rosiglitazone可阻止铁死亡。 | |||
|---|---|---|---|---|
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | Rosiglitazone显着增加AMPK的α亚基中苏氨酸172的磷酸化，提高AMP:ATP比值。在一些细胞系中,Rosiglitazone以过氧化物酶体增殖物激活受体γ无关的方式降低胆固醇合成。Rosiglitazone激活两个含α1-和α2-AMPK的配合物，这导致在乙酰辅酶A羧化酶的磷酸化显着增加。[1] Rosiglitazone激活PPAR-gamma2,充当小鼠骨髓在体外的成骨细胞生成的主导抑制剂。[2] Rosiglitazone增加脂联素从网膜细胞的分泌高达2.3倍，而从皮下脂肪细胞的分泌不受影响。[3] 在3T3-L1脂肪细胞中，Rosiglitazone改变线粒体的形态学特征和蛋白质图谱。[4] |
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| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | Cyclin D1 / CDK2 / CDK4 / Bax / Bcl-2 |
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29725405 | |
| Immunofluorescence | PPARγ / E-cadherin |
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27145370 | |
| Growth inhibition assay | Cell viability |
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29725405 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | Rosiglitazone给药的结果会造成显著的骨丢失，包括减少骨量，骨小梁宽度和骨小梁数量，并增加骨小梁间距。Rosiglitazone也导致骨形成率的降低，同时导致骨髓中的脂肪含量增加。Rosiglitazone减少成骨细胞特异性基因Runx2/Cbfa1，DLX5，以及α1（I）胶原蛋白的表达，而脂肪细胞特异性脂肪酸结合蛋白AP2的表达是增加的。[2] Rosiglitazone上调ob/ob小鼠中白色脂肪细胞中编码线粒体蛋白的基因转录，伴随线粒体数量和线粒体结构的改变。[4] |
|
|---|---|---|
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT02737709 | Terminated | Non-small Cell Lung Cancer |
Sun Yat-sen University |
March 2016 | Phase 2 |
| NCT01402076 | Completed | Healthy Volunteers |
Vanda Pharmaceuticals |
August 2011 | Phase 1 |
| NCT01100619 | Completed | Papillary Thyroid Cancer|Follicular Thyroid Cancer|Huerthle Cell Thyroid Cancer|Renal Cell Carcinoma |
Exelixis |
April 2010 | Phase 1 |
| NCT01415128 | Completed | Erectile Dysfunction |
VIVUS LLC |
April 2010 | Phase 1 |
| NCT01376063 | Completed | Healthy Adult Subjects |
FibroGen |
March 2010 | Phase 1 |
化学信息&溶解度
| 分子量 | 357.43 | 分子式 | C18H19N3O3S |
| CAS号 | 122320-73-4 | SDF | Download Rosiglitazone SDF |
| Smiles | CN(CCOC1=CC=C(C=C1)CC2C(=O)NC(=O)S2)C3=CC=CC=N3 | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 71 mg/mL ( (198.64 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble Ethanol : 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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