Apararenone (MT-3995) is a novel non-steroidal mineralocorticoid receptor antagonists under development for the treatment of diabetic nephropathies and non-alcoholic steatohepatitis.
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描述 | The mineralocorticoid receptor (MR) is a member of the nuclear receptor superfamily and is essential for controlling sodium transport in epithelial tissues such as the kidney and colon[2]. Apararenone is a novel non-steroidal MR antagonist in late-stage clinical trials in patients with heart failure, chronic kidney disease (CKD), hypertension and liver disease[3]. In patients with stage 2 diabetic nephropathy (DN), mean urine albumin to creatine ratio (UACR), as a percentage of baseline, decreased to 62.9%, 50.8%, and 46.5% in the 2.5 mg, 5 mg, and 10 mg apararenone groups, respectively, at week 24. UACR remission rates at week 24 were 0.0%, 7.8%, 29.0%, and 28.1% in the placebo and apararenone 2.5 mg, 5 mg, and 10 mg groups, respectively. Estimated glomerular filtration rate (eGFR) tended to decrease and serum potassium tended to increase[4]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.74mL 0.55mL 0.27mL |
13.72mL 2.74mL 1.37mL |
27.44mL 5.49mL 2.74mL |
CAS号 | 945966-46-1 |
分子式 | C17H17FN2O4S |
分子量 | 364.391 |
别名 | MT-3995 |
运输 | 蓝冰 |
存储条件 |
粉末 Inert atmosphere,Room Temperature 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 120 mg/mL(329.32 mM),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 |
动物实验配方 |