Tropifexor
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货号：A708662
同义名：
LJN452
Tropifexor 是一种 FXR 激动剂，EC50 为 0.26 nM。
Tropifexor 化学结构
Tropifexor 3D分子结构
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Tropifexor 纯度/质量文件 产品仅供科研
货号：A708662
标准纯度：
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产品说明书
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Tropifexor 质控信息
Tropifexor 生物活性
描述
Tropifexor is a novel and highly potent agonist of FXR with EC50 values of 0.2nM and 0.26nM in a HTRF assay and in a BSEP-luc assay, respectively. Tropifexor induced a robust and dose-dependent increase of FXR target genes BSEP (1nM-1μM) and SHP (10nM-1μM) on mRNA level in rat primary hepatocytes exposure to Tropifexor post 24h. Similar increased expression of this two genes could be observed in vivo in the liver of rat orally dosed of Tropifexor at 1mg/kg, as well as increased FGF15 in rat ileum. The dose-dependent decrease of CYP8B1 in rat liver could be observed in rats orally administrated of Tropifexor at doses ranging in 0.01-3mg/kg once daily for 14 days. Also, it led a dose-dependent decrease of serum triglycerides at doses ranging in 0.03-3mg/kg on day 15, at 24 h following oral administration of the compound once daily for 14 days[3]
作用机制
Tropifexor can bind to FXR ligand binding domain (PDB 3DCT).
Tropifexor 动物研究
Dose
Mice: 0.1 mg/kg - 0.9 mg/kg[2] [1] [1]
Administration
p.o., i.v.
Pharmacokinetics
Animal
Mice[1]
Rats[1]
Dogs[1]
Dose
5 mg/kg (i.v.)
3 mg/kg (i.v.)
0.5 mg/kg (i.v.)
Administration
i.v.
i.v.
i.v.
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.)
Tropifexor 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.
Tropifexor 实验方案
计算器
摩尔计算器
总药量计算器
工作液计算器
存储液制备
1mg
5mg
10mg
1 mM
5 mM
10 mM
1.66mL
0.33mL
0.17mL
8.28mL
1.66mL
0.83mL
16.57mL
3.31mL
1.66mL
Tropifexor 技术信息
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