store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Pexacerfont (BMS-562086) 是一种选择性的促肾上腺皮质激素释放因子 (CRF1) 受体拮抗剂,作用于人 CRF1 受体,IC50 为 6.1±0.6 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 461 | 现货 | ||
5 mg | ¥ 1,160 | 现货 | ||
10 mg | ¥ 1,660 | 现货 | ||
25 mg | ¥ 3,550 | 现货 | ||
50 mg | 特惠询价 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,250 | 现货 |
产品描述 | Pexacerfont (BMS-562086) is a selective antagonist of the corticotropin-releasing factor receptor (IC50: 6.1±0.6 nM for the human CRF1 receptor). |
靶点活性 | human CRF1 receptor:6.1±0.6 nM |
体外活性 | Pexacerfont shows an effective and specific inhibitory effect (IC50=6.1 ± 0.6 nM) toward the human CRF1 receptor. It also has greater than 1000-fold lower affinity (IC50>1000 nM) for the CRF-binding protein and biogenic amine receptors[1]. |
体内活性 | Pexacerfont is active in rats (1-10 mg/kg, orally) in the defensive withdrawal and elevated plus-maze models of anxiety. The CLp of Pexacerfont was higher in rats (17.9 mL/kg per min) and dogs (11.6 mL/kg per min) than in chimpanzees (2.0 mL/kg per min). The plasma Pexacerfont concentrations exhibited a multiexponential decline in rats, dogs, and chimpanzees after the intravenous bolus dose. Assuming the value of CLp of Pexacerfont approximates the value of CLb in these three species, Pexacerfont has an estimated hepatic extraction ratio of 0.32, 0.38, and 0.08 in rats, dogs, and chimpanzees, respectively (calculated by dividing CLp by respective hepatic blood flow, 55.2, 30.9, and 25.5 mL/kg per min for rats, dogs, and chimpanzees). The assumption that CLb is equal to CLp is reasonable at least in rats, where the blood to the plasma concentration ratio of BMS-562086-equivalent radioactivity was 0.95 at 1 h postdose[1]. |
别名 | BMS-562086 |
分子量 | 340.42 |
分子式 | C18H24N6O |
CAS No. | 459856-18-9 |
store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 45mg/mL (132.2mM), sonification is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.9375 mL | 14.6877 mL | 29.3755 mL | 73.4387 mL |
5 mM | 0.5875 mL | 2.9375 mL | 5.8751 mL | 14.6877 mL | |
10 mM | 0.2938 mL | 1.4688 mL | 2.9375 mL | 7.3439 mL | |
20 mM | 0.1469 mL | 0.7344 mL | 1.4688 mL | 3.6719 mL | |
50 mM | 0.0588 mL | 0.2938 mL | 0.5875 mL | 1.4688 mL | |
100 mM | 0.0294 mL | 0.1469 mL | 0.2938 mL | 0.7344 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。
Pexacerfont 459856-18-9 GPCR/G Protein CRFR BMS 562086 BMS-562086 BMS562086 Inhibitor inhibitor inhibit