Nidufexor is a potent farnesoid X receptor (FXR) agonist for the treatment of non-alcoholic steatohepatitis (NASH) and hepatobiliary disorders.
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描述 | The farnesoid X receptor (FXR) is a bile acid (BA)-activated nuclear receptor highly expressed in the liver, gall bladder, intestines, and kidney that regulates BA production, conjugation, and transport. Nidufexor is a novel FXR agonist for the treatment of nonalcoholic steatohepatitis (NASH). In adult male Wistar Han rats (age approximately 10 weeks), nidufexor exhibited moderate Cmax (4.5, 12.4, 28.1, 80.9, and 140.8 μM) and terminal elimination half-lives (t1/2; 3.9, 5.7, 6.3, 5.6, 6.3 h) following oral administration (3, 10, 30, 100, and 300 mg/kg). Following intravenous administration (mouse 3.0, rat 5.0 and, dog 0.5 mg/kg), nidufexor exhibited t1/2 values of 4.5, 4.4 and 6.8 h for mouse, rat and dog, respectively. While following oral administration (mouse 10, rat 10 and, dog 2 mg/kg), nidufexor exhibited t1/2 values of 3.5, 2.7 and 10.1 h for mouse, rat and dog, respectively. Nidufexor has advanced to Phase 2 human clinical trials in patients with NASH and diabetic nephropathy[1]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.05mL 0.41mL 0.20mL |
10.25mL 2.05mL 1.02mL |
20.49mL 4.10mL 2.05mL |
CAS号 | 1773489-72-7 |
分子式 | C27H22ClN3O4 |
分子量 | 487.934 |
别名 | LMB763 |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Sealed in dry,Store in freezer, under -20°C |
溶解度 |
DMSO: 85 mg/mL(174.2 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 |
动物实验配方 |