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Zibotentan

CAS No. : 186497-07-4

MCE 站：Zibotentan

产品活性：Zibotentan (ZD4054) 是一种有效的，选择性的，具有口服活性的内皮素 A (ET_A) 受体拮抗剂，K_i 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。

研究领域：GPCR/G Protein  |  Apoptosis

作用靶点：Endothelin Receptor  |  Apoptosis

In Vitro: 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.
Zibotentan (48 hours) treatment increases the number of early apoptotic cells in serum-starved A2780 WT cells.
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.
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..
Zibotentan (ZD4054; 1 μM) decreases the endogenous ET-1-induced phosphorylation/activation of both kinases (AKT and p42/44MAPK) in HEY cells.
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).

In Vivo: Zibotentan (10 mg/kg; intraperitoneal injection; daily; for 21 days) treatment significantly inhibits tumor growth in mice. And Zibotentan treatment increases E-cadherin expression.

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