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Apararenone

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Chemical Structure| 945966-46-1 同义名 : MT-3995
CAS号 : 945966-46-1
货号 : A1005249
分子式 : C17H17FN2O4S
纯度 : 97%
分子量 : 364.391
MDL号 : MFCD31657369
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：
生物活性
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].
实验方案
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
参考文献

[1]Kolkhof P, et al. 30 YEARS OF THE MINERALOCORTICOID RECEPTOR: Mineralocorticoid receptor antagonists: 60 years of research and development. J Endocrinol. 2017 Jul;234(1):T125-T140.

[2]Yang J, Young MJ. The mineralocorticoid receptor and its coregulators. J Mol Endocrinol. 2009 Aug;43(2):53-64.

[3]Kolkhof P, Bärfacker L. 30 YEARS OF THE MINERALOCORTICOID RECEPTOR: Mineralocorticoid receptor antagonists: 60 years of research and development. J Endocrinol. 2017 Jul;234(1):T125-T140.

[4]Wada T, Inagaki M, Yoshinari T, Terata R, Totsuka N, Gotou M, Hashimoto G. Apararenone in patients with diabetic nephropathy: results of a randomized, double-blind, placebo-controlled phase 2 dose-response study and open-label extension study. Clin Exp Nephrol. 2020 Sep 24.