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Tropifexor

Tropifexor

产品编号 T4379   CAS 1383816-29-2
别名: LJN452

Tropifexor (LJN452) 是一种新型的高效 FXR 激动剂,EC50 为 0.2 nM。

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Tropifexor Chemical Structure
Tropifexor, CAS 1383816-29-2
规格 价格/CNY 货期 数量
1 mg ¥ 871 现货
5 mg ¥ 1,730 现货
10 mg ¥ 2,650 现货
25 mg ¥ 4,680 现货
50 mg ¥ 7,230 现货
100 mg ¥ 9,750 现货
200 mg ¥ 12,900 现货
500 mg ¥ 19,500 现货
1 mL * 10 mM (in DMSO) ¥ 2,280 现货
产品目录号及名称: Tropifexor (T4379)
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纯度: 99.85%
纯度: 99.3%
纯度: 99.1%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Tropifexor (LJN452) is a novel and highly potent agonist of FXR with an EC50 of 0.2 nM.
靶点活性 FXR:EC50: 0.2 nM
体外活性 Robust induction of both BSEP and SHP genes is observed in primary cells by Tropifexor in a concentration-dependent manner. BSEP induction above vehicle (DMSO) control is observed at concentrations as low as 1 nM, while strong induction of SHP (15-fold above vehicle) is observed at 10 nM and modest induction of SHP at 1 nM (3-fold).
体内活性 Treatment of rats with Tropifexor exhibits a clear increase in plasma FGF15 protein in a dose-dependent manner, with maximal levels of FGF15 detected at 7 h postdose. Treatment with Tropifexor for 14 days results in a robust dose-dependent reduction in serum triglycerides and reaches a maximal response with a 0.3 mg/kg dose, causing a decrease of triglyceride levels to approximately 79% below the vehicle control group. Tropifexor (compound 1) demonstrates highly potent induction of SHP and FGF15 in the ileum as doses as low as 0.1 mg/kg. In the liver, robust induction of SHP is observed at 0.01 mg/kg of Tropifexor with maximal levels of gene induction achieved at 0.3 mg/kg. Expression of CYP8B1 mRNA following 14 day treatment with Tropifexor is already apparent at the lowest dose (0.003 mg/kg), and CYP8B1 gene expression is fully repressed at doses above 0.03 mg/kg.
细胞实验 Primary rat hepatocytes are plated in 24 well plates and incubated with a 5 point dose response of Tropifexor (compound 1) for 24 hours. RNA is harvested from the cells using the RNeasy 96 kit. Quantitative PCR is performed. The fold change of the transcript over no stimulation is calculated using the ΔΔCt method, with DMSO (vehicle control) being no stimulation.
动物实验 Adult male wild-type Sprague-Dawley rats are used in this study. All animals are fasted for 3 hours before oral dosing with Tropifexor (compound 1) or with vehicle. Tropifexor is administered orally using a range of four doses (0.03, 0.1, 0.3, and 1.0 mg/kg) and compare directly to the vehicle control group (vehicle: 0.5% methylcellulose, 0.5% Tween 80, 99% water, suspension). Animals are sacrificed seven hours after dosing using CO2, liver, ileum and whole blood (in heparinized tubes) samples are collected for analysis.
别名 LJN452
分子量 603.58
分子式 C29H25F4N3O5S
CAS No. 1383816-29-2

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 80 mg/mL(132.5 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.6568 mL 8.2839 mL 16.5678 mL 41.4195 mL
5 mM 0.3314 mL 1.6568 mL 3.3136 mL 8.2839 mL
10 mM 0.1657 mL 0.8284 mL 1.6568 mL 4.142 mL
20 mM 0.0828 mL 0.4142 mL 0.8284 mL 2.071 mL
50 mM 0.0331 mL 0.1657 mL 0.3314 mL 0.8284 mL
100 mM 0.0166 mL 0.0828 mL 0.1657 mL 0.4142 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Tully DC,etal.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.
Coniferaldehyde Linifanib Pepstatin SR9011 (-)-Epicatechin gallate Galangin Mdivi-1 3-Bromopyruvic acid

相关化合物库

该产品包含在如下化合物库中:
含氟化合物库 临床期小分子药物库 已知活性化合物库 表型筛选靶点鉴定库 活性脂质化合物库 脂代谢化合物库 NO PAINS 化合物库 代谢化合物库 药物功能重定位化合物库 抗代谢疾病化合物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
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% ddH2O
计算 重置

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Tropifexor 1383816-29-2 Autophagy Metabolism FXR Inhibitor LJN452 NR1H4 LJN-452 LJN 452 inhibit inhibitor

 

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