store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Bamirastine 抑制配体结合到重组人组胺 H1 受体 (rhH1R),IC50 值为 17.3 nM。Bamirastine 对过敏性皮肤炎症有抑制作用。
产品描述 | Bamirastine inhibits ligand binding to recombinant human histamine H1 receptor (rhH1R) with an IC50 value of 17.3 nM.Bamirastine has an inhibitory effect on allergic skin inflammation. |
靶点活性 | H1 receptor (recombinant human):17.3 nM |
体外活性 | In a concentration-dependent manner, Bamirastine (TAK-427) reduces the specific binding of [3H] pyrilamine to recombinant human H1 receptors (rhH1R) with an IC50 value of 17.3 nM. The calculated Ki value for this interaction is 7.35 nM. Notably, the affinity of Bamirastine is determined to be as high as that of azelastine, 2 times lower than that of Epinastine, 8 times lower than that of ketotifen, and 3 times higher than that of Terfenadine[1]. |
体内活性 |
Bamirastine (TAK-427) exhibits inhibition of histamine-induced skin reactions in guinea pigs and mice, with ID50 values of 0.884 and 0.450 mg/kg, p.o., respectively. Notably, significant inhibition persists 24 hours after dosing in guinea pigs even at a dose of 10 mg/kg. However, even at a high dose of 300 mg/kg, Bamirastine does not affect pentobarbital-induced sleeping time in mice. Furthermore, Bamirastine significantly inhibits passive cutaneous anaphylaxis (PCA) in both mice and guinea pigs. Additionally, it inhibits antigen-induced immediate skin reactions (ISRs) in guinea pigs[1]. |
别名 | TAK-427 |
分子量 | 527.66 |
分子式 | C31H37N5O3 |
CAS No. | 215529-47-8 |
store at low temperature | 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。
Bamirastine 215529-47-8 GPCR/G Protein Immunology/Inflammation Neuroscience Histamine Receptor TAK427 TAK-427 TAK 427 Inhibitor inhibitor inhibit