Zoledronic acid (Zoledronate)
别名: ZA, CGP-4244, GP42446A, ZOL 446 中文名称：唑来膦酸
Zoledronic acid (Zoledronate), 破骨细胞抑制剂，通过抑制甲羟戊酸途径诱导破骨细胞凋亡，并防止小GTP结合蛋白，如Ras 和 Rho的异戊二烯化。Zoledronic acid (ZA) 还可诱导自噬。
Zoledronic acid (Zoledronate) Chemical Structure
CAS: 118072-93-8
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Zoledronic acid (Zoledronate)相关产品
相关信号通路图
Ras抑制剂选择性比较
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 |
|---|---|---|---|---|---|
| J774A.1 | Antiproliferative assay | 100 uM | 72 hrs | Antiproliferative activity against mouse J774A.1 cells assessed as reduction in cell viability at 100 uM after 72 hrs by WST8 assay | 30216851 |
| RAW264.7 | Antiproliferative assay | 100 uM | 72 hrs | Antiproliferative activity against mouse RAW264.7 cells assessed as reduction in cell viability at 100 uM after 72 hrs by WST8 assay | 30216851 |
| MG63 | Antiproliferative assay | 100 uM | 72 hrs | Antiproliferative activity against human MG63 cells assessed as reduction in cell viability at 100 uM after 72 hrs by WST8 assay | 30216851 |
| PC3 | Antiproliferative assay | 100 uM | 72 hrs | Antiproliferative activity against human PC3 cells assessed as reduction in cell viability at 100 uM after 72 hrs by WST8 assay | 30216851 |
| RAW264.7 | Antiproliferative assay | 100 uM | 72 hrs | Antiproliferative activity against RANKL-differentiated mouse RAW264.7 cells assessed as reduction in cell viability at 100 uM after 72 hrs by CCK8 assay | 30216851 |
| MC3T3-E1 | Function assay | 30 to 50 nM | 10 to 15 days | Induction of mineralization in mouse MC3T3-E1 cells at 30 to 50 nM after 10 to 15 days by alizarin red dye based assay | 30216851 |
| C57BL mouse bone marrow cells | Function assay | 50 nM | 10 to 15 days | Induction of mineralization in C57BL mouse bone marrow cells at 50 nM supplemented with fresh medium containing compound every 3 days for 10 to 15 days by alizarin red dye based assay | 30216851 |
| C57BL mouse bone marrow cells/human PC3 cells | Function assay | 50 to 100 nM | 10 to 15 days | Induction of mineralization in C57BL mouse bone marrow cells co-cultured with human PC3 cells at 50 to 100 nM supplemented with fresh medium containing compound every 3 days for 10 to 15 days by alizarin red dye based assay | 30216851 |
| RPMI8226 | Function assay | 0.5 uM | Inhibition of GGPPS in human RPMI8226 cells assessed as reduction in Rap1A prenylation at 0.5 uM by Western blot analysis | 30016091 | |
| BL21(DE3) | Function assay | 30 mins | Inhibition of His6-tagged human truncated FPPS (6-353) expressed in Escherichia coli BL21(DE3) cells using geranyl diphosphate and isopentenyl diphosphate as substrate preincubated with enzyme for 30 mins by spectrophotometric analysis, IC50=0.1μM | 23610597 | |
| BL2-codon plus (DE3) RIL | Function assay | 30 mins | Inhibition of N-terminal His6-tagged Plasmodium vivax GGPPS expressed in Escherichia coli BL2-codon plus (DE3) RIL cells using geranyl diphosphate and isopentenyl diphosphate as substrate preincubated with enzyme for 30 mins by spectrophotometric analysis, IC50=0.13μM | 23610597 | |
| RPMI8226 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human RPMI8226 cells after 72 hrs by MTT assay, EC50=11μM | 23998921 | |
| MCF7 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay, IC50=23μM | 24928399 | |
| Vgamma9/Vdelta2 T-cells | Function assay | 18 hrs | Binding affinity to butyrophilin 3A1 in human Vgamma9/Vdelta2 T-cells assessed as activation of Vgamma9/Vdelta2 T-cells by upregulation of CD69 and CD25 after 18 hrs, EC50=0.4866μM | 29457898 | |
| RPMI8226 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human RPMI8226 cells after 72 hrs by MTT assay, EC50=11μM | 30016091 | |
| RAW264.7 | Function assay | 72 hrs | Inhibition of RANKL-induced osteoclastogenesis in mouse RAW264.7 cells after 72 hrs by TRAP staining based microscopic analysis | 30216851 | |
| K562 | Function assay | 240 mins | Activation of butyrophilin 3A1 in human K562 cells assessed as interferon-gamma production pretreated for 240 mins followed by HMBPP-treated Vgamma9Vdelta2 T cells addition and measured after 20 hrs by ELISA, EC50=23μM | 31531198 | |
| MIAPaCa2 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human MIAPaCa2 cells assessed as decrease in cell growth measured after 72 hrs by MTT assay, EC50=13.4μM | 31725297 | |
| PANC1 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human PANC1 cells assessed as decrease in cell growth measured after 72 hrs by MTT assay, EC50=16.1μM | 31725297 | |
| HFF cells | Function assay | Inhibitory concentration against the growth of Toxoplasma gondii overexpressing FPPS enzyme in human foreskin fibroblast monolayer cells; (control = 0.60 uM, experiment 1), IC50=7.8μM | 15857119 | ||
| HFF cells | Function assay | In vitro inhibitory concentration against the growth of Toxoplasma gondii in human foreskin fibroblast monolayer cells (HFF cells), IC50=0.79μM | 15857119 | ||
| Gamma delta T cells | Function assay | Effective concentration against human Gamma delta T cells, EC50=5.4μM | 15828834 | ||
| human SF-268 cell | Proliferation assay | Antiproliferative activity against human SF-268 cell line by MTT assay, IC50=14.3 μM | 16970405 | ||
| human NCI-H460 cell | Proliferation assay | Antiproliferative activity against human NCI-H460 cell line by MTT assay, IC50=11.7 μM | 16970405 | ||
| HFF cells | Function assay | Inhibitory concentration against the growth of Toxoplasma gondii overexpressing FPPS enzyme in human foreskin fibroblast monolayer cells; (control = 0.79 uM, experiment 3), IC50=7.8μM | 15857119 | ||
| HFF cells | Function assay | Inhibitory concentration against the growth of Toxoplasma gondii overexpressing FPPS enzyme in human foreskin fibroblast monolayer cells; (control = 1.1 uM, experiment 2), IC50=8.3μM | 15857119 | ||
| BT-549 | Antitumor assay | Antitumor activity against human BT-549 cells xenografted SCID mouse co-transfected with human gamma delta T lymphocytes assessed as survival time prolongation at 2 ug, ip coadministered with human recombinant IL2 | 18937434 | ||
| BT-549 | Antitumor assay | Antitumor activity against human BT-549 cells xenografted SCID mouse co-transfected with human gamma delta T lymphocytes assessed as survival time prolongation at 5 ug, ip coadministered with human recombinant IL2 | 18937434 | ||
| J774 | Cytotoxicity assay | Cytotoxicity against mouse J774 cells assessed as reduction in cell viability, IC50=7.8μM | 24813742 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Zoledronic acid (Zoledronate), 破骨细胞抑制剂，通过抑制甲羟戊酸途径诱导破骨细胞凋亡，并防止小GTP结合蛋白，如Ras 和 Rho的异戊二烯化。Zoledronic acid (ZA) 还可诱导自噬。 | ||
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| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | Zoledronic acid (10 µM和100 µM)引起MCF-7细胞按比例显著减少(49.54% ，对照组23.55% ) (P < 0.05)。Zoledronic acid在0.1–10 µM浓度下对MDA-MB-231细胞影响很小，然而在100 µM浓度下会导致细胞数量显著降低。Zoledronic acid (100 µM)在72小时时会引起MCF-7细胞数减少63.5%，在96小时时，会使其减少87.1%。Zoledronic acid (10 µM)会导致MCF-7细胞凋亡多于4倍的增加，而在100 µM浓度下，会使细胞凋亡的比例增加6倍。Zoledronic acid (10 µM) 和paclitaxel (2 µM)引起的细胞凋亡（对照组的774.8%）与单独使用zoledronic acid（155.71%）相比增加了5倍，与单独使用paclitaxel（189.68）相比，增加了4倍。Zoledronic acid诱导的MCF-7乳腺癌细胞凋亡会被甲羟戊酸途径中间体的加入所抑制，这与在破骨细胞，巨噬细胞和骨髓瘤细胞中的情况相一致。[1] Zoledronic acid剂量依赖性增强OPG基因的表达和人类成骨细胞（hOB）中蛋白质的分泌，在10 nM浓度下，72小时后有最大效果，这与Zoledronic acid更高的生物学效能相一致。Zoledronic acid阻止了人类成骨细胞中糖皮质激素dexamethasone对OPG mRNA和蛋白质合成的抑制作用。Zoledronic acid在人类成骨细胞中分别诱导2倍的I型胶原分泌和4倍的碱性磷酸酶活性。[2] |
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| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | ALDH1 / Oct4 / Nanog / Sox2 / CD49f N-cadherin / E-cadherin / Vimentin |
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30791957 | |
| Growth inhibition assay | Cell viability |
|
30791957 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 |
在5T2MM小鼠体内，Zoledronic acid（120毫克/千克，皮下注射）防止损伤的形成，防止松质骨和骨密度损失，并且减少破骨细胞的范围。在5T2MM小鼠体内，Zoledronic acid（120毫克/千克，皮下注射）也减少了病变蛋白浓度和肿瘤负担以及血管新生。[3] |
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|---|---|---|
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT05743179 | Recruiting | Hip Fractures|Pneumonia |
The University of Hong Kong|Queen Mary Hospital Hong Kong|Caritas Medical Centre Hong Kong|Prince of Wales Hospital Shatin Hong Kong|United Christian Hospital |
December 5 2022 | Phase 4 |
| NCT04957641 | Completed | Hereditary Angioedema |
Takeda |
April 21 2022 | -- |
| NCT05213286 | Recruiting | Autism Spectrum Disorder|Schizotypal Disorder |
Glostrup University Hospital Copenhagen |
February 1 2022 | Not Applicable |
化学信息&溶解度
| 分子量 | 272.09 | 分子式 | C5H10N2O7P2 |
| CAS号 | 118072-93-8 | SDF | Download Zoledronic acid (Zoledronate) SDF |
| Smiles | C1=CN(C=N1)CC(O)(P(=O)(O)O)P(=O)(O)O | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
0.1M NAOH : 25 mg/mL (91.88 mM) Water : 0.5 mg/mL (1.83 mM) Warmed with 50℃ water bath; Ultrasonicated; DMSO : Insoluble ( ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) |
摩尔浓度计算器 |
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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）
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）
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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* 必填项
常见问题及建议解决方法
问题 1:
How can I reconstitute the compound for in vivo studies?
回答：
Please dissolve this compound directly to 30% PEG400+0.5% Tween80+5% Propylene glycol.
