Zibotentan
N-(3-Methoxy-5-Methylpyrazin-2-Yl)-2-[4-(1,3,4-Oxadiazol-2-Yl)Phenyl]Pyridine-3-Sulfonamide
CAS: 186497-07-4
Molecular Formula: C19H16N6O4S
Zibotentan - Names and Identifiers
Zibotentan - Physico-chemical Properties
| Molecular Formula | C19H16N6O4S |
| Molar Mass | 424.43 |
| Density | 1.422 |
| Melting Point | 239 - 241°C |
| Boling Point | 637.0±65.0 °C(Predicted) |
| Solubility | DMSO (Sparingly), Methanol (Slightly) |
| Appearance | Solid |
| Color | White to Off-White |
| pKa | 5.62±0.40(Predicted) |
| Storage Condition | Sealed in dry,Store in freezer, under -20°C |
| In vitro study | In human and rat smooth muscle cells, Zibotentan specifically inhibits the anti-apoptotic effect mediated by ET A, but has no effect on the pro-apoptotic effect mediated by ET B, zibotentan binds with high affinity to endothelin A receptor (ET A) with A K I of 13 nM, whereas it has no affinity to endothelin B receptor (ETB) with an IC50>10 μm. In ovarian cancer cell lines HEY and OVCA 433, which secrete ET-1 and express ET A and ET B mRNA, 1 μm Zibotentan treatment inhibited ET-1-Induced Mitogenic activity. ZD4054 (1 μm) inhibited ET-1-induced EGFR Transactivation In HEY and OVCA 433 cells. Zibotentan (1 μm), by enhancing E-cadherin expression and promoter activity, and inhibiting vascular endothelial growth factor (VEGF) secretion and invasion in 433 cells reversal of ET-1-mediated epithelial-mesenchymal transition (EMT). Zibotentan also potently inhibits basal and ET-1-induced cell proliferation in SKOV-3 and A- 2780 cells, which correlates with inhibition of AKT and p42/44MAPK phosphorylation, it is also associated with the inhibition of bcl-2 and caspase-3 with the activation of the poly (ADP-RIBOSE) POLYMERASE PROTEIN, leading to increased APOPTOSIS. |
| In vivo study | Zibotentan(10 mg/kg/day) administration for 21 days effectively inhibited the growth of 69% of HEY ovarian cancer xenografts in mice without associated toxicity, this correlates with a 37% inhibition of Ki-67 expression and 62% inhibition of tumor-induced angiogenesis of cell proliferation. Similarly, Zibotentan treatment significantly inhibited the expression of matrix metalloproteinase-2 (MMP-2) and VEGF, as well as the activation of p42/44 MAPK and EGFR, and effectively enhanced the expression of E-cadherin. |
Zibotentan - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.356 ml | 11.781 ml | 23.561 ml |
| 5 mM | 0.471 ml | 2.356 ml | 4.712 ml |
| 10 mM | 0.236 ml | 1.178 ml | 2.356 ml |
| 5 mM | 0.047 ml | 0.236 ml | 0.471 ml |
Last Update：2024-01-02 23:10:35
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Product Name: Zibotentan (ZD4054) Visit Supplier Webpage Request for quotation
CAS: 186497-07-4
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 186497-07-4
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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