Clazosentan

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Clazosentan (Ro 61-1790) 是一种选择性的内皮素 A 受体 (ETA receptor) 拮抗剂。Clazosentan 抑制 ET-1 介导的血管收缩。Clazosentan 可预防脑血管痉挛、血管痉挛相关性脑梗死。

Clazosentan (Ro 61-1790) is a selective endothelin A (ETA) receptor antagonist. Clazosentan inhibits ET-1-mediated vasoconstriction. Clazosentan prevents cerebral vasospasm, vasospasm-related cerebral infarction.

Clazosentan (0.1 μM) inhibits the ETA receptor in cerebral arteries.Clazosentan is a substrate of the organic anion-transporting polypeptide (OATP) 1B1/1B3.

Clazosentan (10 μM, 0.05?mL/kg, intracisternal injection) inhibits the contractile responses to ET-1 in rats.Clazosentan (10 mg/kg, s.c.) inhibits IL-33-induced hypernociception in mice.Animal Model:RatsDosage:10 μM, 0.05?mL/kg Administration: Intracisternal injection Result:Inhibited the contractile responses to ET-1, without preventing SAH-induced upregulation of ET receptors in cerebral arteries.

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GPCR/G Protein

Endothelin Receptor

Endothelin Receptor

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180384-56-9

577.57

C25H23N9O6S

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 83.33 mg/mL (144.28 mM; 超声助溶 )

COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(nc1OCCO)-c1ccnc(c1)-c1nn[nH]n1

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(-20℃)

With Ice Pack

≥ 2 years