| Bioactivity | Zibotentan (ZD4054) is a potent, selective and orally active endothelin A (ETA) receptor antagonist with a Ki of 13 nM. Zibotentan has no inhibitory effect on ETB. Zibotentan has anticancer effects and can be used for castration-resistant prostate cancer (CRPC) research[1][2]. | ||||||||||||
| Invitro | Zibotentan potently inhibits the binding of 125iodine-ET-1 to cloned human ETA expressed in mouse erythroleukaemic cells, with a pIC50 (concentration to inhibit 50% of binding) value of 22 nM[1].Zibotentan (48 hours) treatment increases the number of early apoptotic cells in serum-starved A2780 WT cells[2].Zibotentan (ZD4054; 1 μM; 24 hours) treatment shows significant inhibition of cell proliferation in serum-starved HEY, OVCA 433, SKOV-3, and A-2780 cells[3].Zibotentan (ZD4054; 1 μM; 48 hours) treatment induces an increase in apoptotic cells. Zibotentan inhibits bcl-2 and activates caspase-3 and poly(ADP-ribose) polymerase proteins.[3].Zibotentan (ZD4054; 1 μM) decreases the endogenous ET-1-induced phosphorylation/activation of both kinases (AKT and p42/44MAPK) in HEY cells[3].Zibotentan treatment also results in a reduction of ETAR-driven angiogenesis and invasive mediators, such as vascular endothelial growth factor, cyclooxygenase-1/2, and matrix metalloproteinase (MMP)[3]. Cell Proliferation Assay[3] Cell Line: | ||||||||||||
| Name | Zibotentan | ||||||||||||
| CAS | 186497-07-4 | ||||||||||||
| Formula | C19H16N6O4S | ||||||||||||
| Molar Mass | 424.43 | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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Zibotentan
CAS: 186497-07-4 F: C19H16N6O4S W: 424.43
Zibotentan (ZD4054) is a potent, selective and orally active endothelin A (ETA) receptor antagonist with a Ki of 13 nM.
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