Eprosartan

Research use only, not for human use.

Eprosartan (SKF-108566J free base) is a selective, competitive nonpeptide angiotensin II receptor antagonist with high affinity for AT1 receptor subtypes, used as an antihypertensive agent.

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 .

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.

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.

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Endocrinology/Hormones

RAAS

RAAS

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133040-01-4

424.51

C23H24N2O4S

>98% (HPLC)

In Vitro:?DMSO : 125 mg/mL (294.46 mM; Ultrasonic )

CCCCc1ncc(\C=C(/Cc2cccs2)C(O)=O)n1Cc1ccc(cc1)C(O)=O

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(-20℃)

With Ice Pack

≥ 2 years