Esaxerenone (CS-3150) 是一种高度有效且有选择性的非类固醇盐皮质激素受体拮抗剂。

Esaxerenone (CS-3150) is a highly potent and selective non-steroidal mineralocorticoid receptor antagonist.

Solid

Mineralocorticoid receptor

After single oral administration of Esaxerenone at 0.1, 0.3, 1, and 3?mg/kg, maximum plasma concentration (C max ) and the area under the plasma concentration versus time curve (AUC) are increased with dose. Time to reach the maximum plasma concentration (T max ) of Esaxerenone ranges from 2.0 to 4.5?h. After intravenous administration of Esaxerenone at 0.1, 0.3, 1, and 3?mg/kg, the total body clearance (CL) and distribution volume at steady state (V ss ) are 3.53 to 6.69?mL/min/kg and 1.47 to 2.49?L/kg, respectively, in rats, and 2.79 to 3.69?mL/min/kg and 1.34 to 1.54?L/kg, respectively, in cynomolgus monkeys. Up to 168?h after administration, 3.9% and 91.4% of dosed radioactivity are excreted in rat urine and feces, respectively, and 95.2% in total. In monkeys, the excreted radioactivity up to 168?h is 11.5% in urine, 82.3% in feces, and 93.9% in

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Yamada M, et al. Pharmacokinetics, distribution, and disposition of esaxerenone, a novel, highly potent and selective non-steroidal mineralocorticoid receptor antagonist, in rats and monkeys. Xenobiotica. 2017 Dec;47(12):1090-1103.

In Vitro: DMSO : 100 mg/mL (214.38 mM; Need ultrasonic)配制储备液