Powder: -20°C for 3 years | In solvent: -80°C for 1 year
BMS-986251 is a potent and specific RORγt inverse agonist that exerts its action via oral administration. It shows an EC 50 of 12 nM for RORγt GAL4. In human whole blood assay, BMS-986251 effectively inhibits IL-17 with an EC 50 of 24 nM. Furthermore, BMS-986251 exhibits strong therapeutic effects in mouse acanthosis and Imiquimod-induced models, which are commonly used preclinical models for psoriasis.
产品描述 | BMS-986251 is a potent and specific RORγt inverse agonist that exerts its action via oral administration. It shows an EC 50 of 12 nM for RORγt GAL4. In human whole blood assay, BMS-986251 effectively inhibits IL-17 with an EC 50 of 24 nM. Furthermore, BMS-986251 exhibits strong therapeutic effects in mouse acanthosis and Imiquimod-induced models, which are commonly used preclinical models for psoriasis. |
靶点活性 | RORβ:>10 μM (EC50), RORγt:12 nM (EC50), IL-17:24 nM (EC50), RORα:>10 μM (EC50) |
体外活性 | BMS-986251 is against ROR family members (RORα GAL4: EC 50 >10 μM; RORβ GAL4: EC 50 >10 μM) and against other nuclear receptors (PXR: EC 50 >5 μM; LXRα: EC 50 >7.5 μM; LXRβ: EC 50 >7.5 μM). BMS-986251 does not inhibit any of the CYP’s[1]. |
体内活性 | BMS-986251 (5-45 mg/kg; orally; twice daily until day 9) results in reduced ear thickness[1]. BMS-986251 (0.13, 0.79, 4.76 mg/kg; orally; once a day) displays a dose-dependent reduction of the IL-17F produced in na?ve C57BL/6 female mice (7-9 weeks)[1]. BMS-986251 (2 mg/kg of IV and 4 mg/kg of PO) has a T 1/2 of 7.7 hours, a CL of 2.7 mL/min?kg, and a V ss of 1.9 L/kg for IV in mouse[1]. Animal Model: C57BL/6 female mice with acanthosis[1]Dosage: 5, 15, 45 mg/kg Administration: Orally; twice daily until day 9 Result: Resulted in reduced ear thickness and significantly reduces imiquimod (IMQ)-induced skin thickening. Animal Model: Mouse or rat[1]Dosage: 2 mg/kg of IV and 4 mg/kg of PO (Pharmacokinetic Analysis) Administration: IV or PO Result: Had a T 1/2 of 7.7 hours, a CL of 2.7 mL/min?kg, and a V ss of 1.9 L/kg for IV in mouse. Had a C max of 4.8 μM and an AUC of 37 μM?h for PO in mouse. Had a T 1/2 of 11 hours, a CL of 1.3 mL/min?kg, and a V ss of 1.25 L/kg for IV in rat. Had a C max of 4.7 μM and an AUC of 64 μM?h for PO in rat. |
分子量 | 667.61 |
分子式 | C30H29F8NO5S |
CAS No. | 2460133-35-9 |
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。
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