Powder: -20°C for 3 years | In solvent: -80°C for 1 year
RORγt Inverse agonist 10 is a highly potent and orally bioavailable compound that acts as an antagonist for the retinoic acid receptor-related orphan nuclear receptor gamma t (RORγt). With an IC50 of 51 nM, it effectively inhibits the activity of RORγt, a prominent transcription factor involved in the regulation of genes associated with the pathogenesis of psoriasis, including IL-17A, IL-22, and IL-23R.
产品描述 | RORγt Inverse agonist 10 is a highly potent and orally bioavailable compound that acts as an antagonist for the retinoic acid receptor-related orphan nuclear receptor gamma t (RORγt). With an IC50 of 51 nM, it effectively inhibits the activity of RORγt, a prominent transcription factor involved in the regulation of genes associated with the pathogenesis of psoriasis, including IL-17A, IL-22, and IL-23R. |
靶点活性 | RORγt:51 nM (IC50) |
体外活性 | RORγt Inverse agonist 10 has a good liver microsome stability (human CL int =0.010 mL/min/mg, mouse CL int =0.030 mL/min/mg)[1]. RORγt Inverse agonist 10 suppresses the IL-17A production in a dose-dependent manner with an IC 50 of 130 nM in a human whole-blood assay[1]. |
体内活性 | RORγt Inverse agonist 10 (3-100 mg/kg; p.o.) shows robust and dose-dependent inhibitory effect on the IL-17A production in mouse IL-18/23-induced cytokine expression model[1]. RORγt Inverse agonist 10 (1.145 mg/kg; p.o.) shows a high AUC of 15000 nM*h and t 1/2 of 3.6 hours[1]. Animal Model: C57/BL6 male mice, mouse IL-18/23-induced cytokine expression model[1]Dosage: 3 mg/kg, 10 mg/kg, 30 mg/kg, 100 mg/kg Administration: Oral administration Result: Significantly inhibited the IL-17A production in a dose-dependent manner. Animal Model: Mice[1]Dosage: 1.145 mg/kg (Pharmacokinetic Analysis) Administration: Oral administration Result: AUC=15000 nM*h, t 1/2 =3.6 hours. |
分子量 | 572.512 |
分子式 | C25H26F6N6O3 |
CAS No. | 2413986-35-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
RORγt Inverse agonist 10 2413986-35-1 RORrt Inverse agonist 10 RORgammat Inverse agonist 10 Inhibitor inhibitor inhibit