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Esaxerenone

CAS No. : 1632006-28-0

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

研究領域：Metabolic Enzyme/Protease  |  Vitamin D Related/Nuclear Receptor

作用靶點：Mineralocorticoid Receptor

In Vivo: 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 total.

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