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描述 | Esaxerenone is recognized as a highly effective and selective antagonist for the non-steroidal mineralocorticoid receptor[1]. |
Animal study | Following a single oral dose of Esaxerenone at 0.1, 0.3, 1, and 3 mg/kg, there is a dose-dependent increase in both the maximum plasma concentration (Cmax) and the area under the plasma concentration-time curve (AUC). The Tmax, or the time to reach Cmax, varies from 2.0 to 4.5 hours. With intravenous doses of Esaxerenone at the same concentrations, the total body clearance (CL) ranges from 3.53 to 6.69 mL/min/kg and the steady-state distribution volume (Vss) from 1.47 to 2.49 L/kg in rats, while in cynomolgus monkeys, the CL is 2.79 to 3.69 mL/min/kg and the Vss is 1.34 to 1.54 L/kg. Post-administration, up to 168 hours, rats excrete 3.9% of the radioactivity in urine and 91.4% in feces, totaling 95.2%. In monkeys, 11.5% is excreted in urine, 82.3% in feces, and 93.9% in total within the same timeframe[1]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.14mL 0.43mL 0.21mL |
10.72mL 2.14mL 1.07mL |
21.44mL 4.29mL 2.14mL |
CAS号 | 1632006-28-0 |
分子式 | C22H21F3N2O4S |
分子量 | 466.473 |
别名 | CS-3150;XL-550 |
运输 | 蓝冰 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Sealed in dry,2-8°C |
溶解方案 |
DMSO: 105 mg/mL(225.09 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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动物实验配方 |