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Esaxerenone
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Esaxerenone图片
CAS NO:1632006-28-0
规格:98%
分子量:466.47
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
Esaxerenone is a novel, highly potent and selective non-steroidal mineralocorticoid receptor antagonist.
CAS:1632006-28-0
分子式:C22H21F3N2O4S
分子量:466.47
纯度:98%
存储:Store at -20°C

Background:

Esaxerenone is a novel, highly potent and selective non-steroidal mineralocorticoid receptor antagonist.


After single oral administration of Esaxerenone at 0.1, 0.3, 1, and 3 mg/kg, maximum plasma concentration (Cmax) and the area under the plasma concentration versus time curve (AUC) are increased with dose. Time to reach the maximum plasma concentration (Tmax) 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 (Vss) 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[1].


参考文献:
[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.