| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| Z408265-1ml |
1ml |
现货  |
|
| 别名 | 紫博腾坦 (ZD4054) |
|---|---|
| 英文别名 | N-(3-methoxy-5-methyl-2-pyrazinyl)-2-[4-(1,3,4-oxadiazol-2-yl)phenyl]-3-pyridinesulfonamide |
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | Zibotentan (ZD4054) |
| 生化机理 | 齐博坦（ZD4054）是一种特异性内皮素（ET）A 拮抗剂，IC50 为 21 nM，对 ETB 无活性。第 3 阶段 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 拮抗剂 |
| 作用机制 | 内皮素受体 ET-A 拮抗剂 |
| 产品介绍 |
Zibotentan (ZD4054) 是一种有效的，选择性的内皮素 A (ETA) 受体拮抗剂，Ki 为 13 nM。Zibotentan 对 ETB 没有抑制作用。Zibotentan 具有抗癌作用，可用于去势抵抗性前列腺癌 (CRPC) 的研究。
Information Zibotentan (ZD4054) Zibotentan (ZD4054) is a specific Endothelin (ET)A antagonist with IC50 of 21 nM, exhibiting no activity at ETB. Phase 3. As Zibotentan specifically inhibits ETA-mediated antiapoptotic effects, but not ETB-mediated proapoptotic effects in human and rat smooth muscle cells, Zibotentan binds to endothelin A receptor (ETA) with high affinity with Ki of 13 nM, and has no affinity for endothelin B receptor (ETB) with IC50 of >10 μM. Zibotentan treatment at 1 μM inhibits ET-1 induced mitogenic activity in ovarian carcinoma cell lines HEY and OVCA 433 secreting ET-1 and expressing ETA and ETB mRNA. ZD4054 (1 μM) inhibits ET-1 induced EGFR transactivation in HEY and OVCA 433 cells. Zibotentan (1 μM) reverts ET-1 mediated epithelial-mesenchymal transition (EMT), by enhancing E-cadherin expression and promoter activity, and inhibiting vascular endothelial growth factor (VEGF) secretion and invasiveness in HEY and OVCA 433 cells. Zibotentan also potently inhibits the basal and ET-1 induced cell proliferation in SKOV-3 and A-2780 cells, associated with the inhibition of AKT and p42/44MAPK phosphorylation, and with increased apoptosis through the inhibition of bcl-2 and activation of caspase-3 and poly(ADP-ribose) polymerase proteins. In vivo Administration of Zibotentan at 10 mg/kg/day for 21 days potently inhibits the growth of HEY ovarian carcinoma xenografts in mice by 69% with no associated toxicity, which is in association with the blocking of cell proliferation evaluated by 37% inhibition of the Ki-67 expression, and the 62% inhibition of tumor-induced vascularization. Consistently, Zibotentan treatment significantly inhibits the expression of matrix metalloproteinase-2 (MMP-2) and VEGF, as well as the activation of p42/44 MAPK and EGFR, and potently enhances the expression of E-cadherin. cell lines：U87, MT330, SJ-G2, and GBM6 human glioma lines Concentrations：Dissolved in DMSO, final concentrations 1 μM Incubation Time：48 hours Powder Purity:≥99% |
| 分子类型 | 小分子 |
|---|---|
| Canonical SMILES | COC1=NC(=CN=C1N[S](=O)(=O)C2=CC=CN=C2C3=CC=C(C=C3)C4=NN=CO4)C |
| 分子量 | 424.43 |
| Concentration | 9-11（mmol/L） |
|---|---|
| Proton NMR spectrum | Conforms to Structure |
首页
400-620-6333
