Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Tropifexor (LJN452) 是一种新型的高效 FXR 激动剂,EC50 为 0.2 nM。
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 80 mg/mL(132.5 mM)
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 |
对于不同动物的给药剂量换算,您也可以参考 更多...
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。
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。
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