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描述 | Excessive activation of mineralocorticoid receptors by the steroid hormones aldosterone or cortisol can lead to the development of cardiovascular disease. Finerenone is a novel, potent, and selective nonsteroidal mineralocorticoid receptor antagonist with IC50 value of 18nM and exhibits no activity at any other steroid hormone receptor and on 65 receptors and ion channels (IC50>10μM). Finerenone showed a favorable PK profile and high oral bioavailability (94%) in rats[1]. Finerenone reduced cardiac hypertrophy, plasma prohormone of brain natriuretic peptide, and proteinuria more efficiently than eplerenone when comparing equinatriuretic doses. It improved systolic and diastolic left ventricular function and reduced plasma prohormone of brain natriuretic peptide levels at dose of 1mg/kg, daily, p.o., in rats that developed chronic heart failure after coronary artery ligation, suggesting that finerenone may offer end-organ protection with a reduced risk of electrolyte disturbances[2]. |
作用机制 | Finerenone fills part of the MR binding pocket between Asn770 and Leu766[1]. |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.64mL 0.53mL 0.26mL |
13.21mL 2.64mL 1.32mL |
26.43mL 5.29mL 2.64mL |
CAS号 | 1050477-31-0 |
分子式 | C21H22N4O3 |
分子量 | 378.424 |
别名 | BAY 94-8862;FIN |
运输 | 蓝冰 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Keep in dark place,Sealed in dry,2-8°C |
溶解方案 |
DMSO: 190 mg/mL(502.08 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 |