CAS No.: 1383816-29-2
Tropifexor Catalog No. CSN23688
Synonyms: LJN452
Tropifexor is a potent agonist of FXR with EC50 of 0.26 nM.
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纯度 & 质量文件
批次:
靶点选择性
生物活性
- 描述
- 作用机制
动物研究 剂量 Mice: 0.1 mg/kg - 0.9 mg/kg[2] (p.o.) Rat: 3 mg/kg[1] (i.v.); 10 mg/kg[1] (p.o.)
给药途径 p.o., i.v.
动物药代数据 Animal Mice[1] Rats[1] Dogs[1] Dose 5 mg/kg (i.v.)
10 mg/kg (p.o.)3 mg/kg (i.v.)
1 mg/kg (p.o.)0.5 mg/kg (i.v.)
2 mg/kg (p.o.)Administration i.v.
p.o.i.v.
p.o.i.v.
p.o.F 9.2% (p.o.) 10% (p.o.) 10% (p.o.) T1/2 2.6 h (i.v.) 3.7 h (i.v.) 7.4 h (i.v.) AUC 4785 h·nM (p.o.) 307 h·nM (p.o.) 3660 h·nM (p.o.) CL 5.3 ml/min/kg (i.v.) 9.3 ml/min/kg (i.v.) 1.5 ml/min/kg (i.v.) Cmax 1186 nM (p.o.) 53 nM (p.o.) 332 nM (p.o.) Protein binding (free drug %) 0.999 0.999 0.999 Vss 0.70 L/kg (i.v.) 0.72 L/kg (i.v.) 0.46 L/kg (i.v.) - 参考文献
- [1] Tully DC, Rucker PV, et al. Discovery of Tropifexor (LJN452), a Highly Potent Non-bile Acid FXR Agonist for the Treatment of Cholestatic Liver Diseases and Nonalcoholic Steatohepatitis (NASH). J Med Chem. 2017 Dec 28;60(24):9960-9973.
- [2] Hernandez ED, Zheng L, et al. Tropifexor-Mediated Abrogation of Steatohepatitis and Fibrosis Is Associated With the Antioxidative Gene Expression Profile in Rodents. Hepatol Commun. 2019 May 17;3(8):1085-1097.
- [3] Tully DC, Rucker PV, Chianelli D, Williams J, Vidal A, Alper PB, Mutnick D, Bursulaya B, Schmeits J, Wu X, Bao D, Zoll J, Kim Y, Groessl T, McNamara P, Seidel HM, Molteni V, Liu B, Phimister A, Joseph SB, Laffitte B. Discovery of Tropifexor (LJN452), a Highly Potent Non-bile Acid FXR Agonist for the Treatment of Cholestatic Liver Diseases and Nonalcoholic Steatohepatitis (NASH). J Med Chem. 2017 Dec 28;60(24):9960-9973. doi: 10.1021/acs.jmedchem.7b00907. Epub 2017 Dec 8. PMID: 29148806.
实验方案
- 计算器
- 储存液制备
技术信息
| CAS号 | 1383816-29-2 | 储存条件 |
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| 分子式 | C29H25F4N3O5S | 运输 | 蓝冰 | |||||
| 分子量 | 603.58 | 别名 | LJN452 | |||||
| 溶解度 |
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动物实验配方 |
