Eprosartan (SKF-108566J free base) 是一种选择性，竞争性，非肽和具有口服活性的血管紧张素 II 受体 (angiotensin II receptor) 拮抗剂，可用作降压剂。Eprosartan 结合血管紧张素 II 受体，在大鼠和人类肾上腺皮质膜中的 IC50 值分别为 9.2 nM 和 3.9 nM。
货号:ajcx33030
CAS:133040-01-4
分子式:C23H24N2O4S
分子量：424.51
溶解度:DMSO : 125 mg/mL (294.46 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

Eprosartan (SKF-108566J free base) is a selective, competitive, nonpeptid and orally active angiotensin II receptor antagonist, used as an antihypertensive. Eprosartan binds angiotensin II receptor with IC50s of 9.2 nM and 3.9 nM in rat and human adrenal cortical membranes, respectively [1].

Eprosartan (SKF-108566J) inhibits [125I]AII binding to human liver membranes (IC50 of 1.7 nM) and to rat mesenteric artery membranes (IC50 of 1.5 nM). In rabbit aortic smooth muscle cells, Eprosartan caused a concentration-dependent inhibition of AII-induced increases in intracellular Ca2+ levels[1].

In conscious normotensive rats, i.v. administration of Eprosartan (0.01-0.3 mg/kg) produced dose-dependent parallel shifts in the AII pressor dose-response curve. Administration of Eprosartan (3-10 mg/kg) intraduodenally or intragastrically to conscious normotensive rats resulted in a dose-dependent inhibition of the pressor response to AII (250 ng/kg, i.v.). At 10 mg/kg, i.d., significant inhibition of the pressor response to AII was observed for 3 hr[1].

[1]. R M Edwards, et al. Pharmacological characterization of the nonpeptide angiotensin II receptor antagonist, SK&F 108566. J Pharmacol Exp Ther. 1992 Jan;260(1):175-81.