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Atrasentan hydrochloride

CAS No. : 195733-43-8

MCE 国际站：Atrasentan hydrochloride

产品活性：Atrasentan hydrochloride (ABT-627 hydrochloride) 是一种有效的选择性 内皮素 A 受体 (endothelin A receptor) 拮抗剂，抑制 ET_A 的活性，IC₅₀ 值为 0.0551 nM。

研究领域：GPCR/G Protein

作用靶点：Endothelin Receptor

In Vitro: Atrasentan hydrochloride (ABT-627 hydrochloride) (0-50 μM) significantly inhibits LNCaP and C4-2b prostate cancer cell growth. Atrasentan profoundly induces several CYPs and drug transporters (e.g. 12-fold induction of CYP3A4 at 50 μM). It is a moderate P-gp inhibitor (IC₅₀ in P388/dx cells=15.1±1.6 μM) and a weak BCRP inhibitor (IC₅₀ in MDCKII-BCRP cells=59.8±11 μM).

In Vivo: Atrasentan hydrochloride (ABT-627 hydrochloride) (3 mg/kg, p.o.) inhibits the pressor response induced by big endothelin-1 (1 nmol/kg) in pithed rats. Aatrasentan (ABT-627, 10 mg/kg, i.p.) inhibits the C4-2b tumor growth within the bone environment to some extent in the SCID-hu model.

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