Powder: -20°C for 3 years | In solvent: -80°C for 1 year
FR167344 free base is an orally active and nonpeptide antagonist of bradykinin receptor B2. FR167344 free base displays a high-affinity binding to the B2 receptor (IC50: 65 nM). It has no binding affinity for the B1 receptor.
产品描述 | FR167344 free base is an orally active and nonpeptide antagonist of bradykinin receptor B2. FR167344 free base displays a high-affinity binding to the B2 receptor (IC50: 65 nM). It has no binding affinity for the B1 receptor. |
靶点活性 | Bradykinin receptor B2:65 nM |
体外活性 | FR167344 shows no stimulatory effects on PI hydrolysis. FR167344 inhibits the B2 receptor-mediated phosphatidylinositol (PI) hydrolysis and produces a concentration-dependent rightward shift in the dose-response curve to bradykinin, in competitive experiments using membranes prepared from Chinese hamster ovary cells expressing the bradykinin receptor subtypes. This shift is accompanied by a progressive reduction of maximal response. Estimated pA2 values for the antagonism of bradykinin-induced PI hydrolysis by FR167344 is 8.0 [1]. |
体内活性 | FR167344 (p.o.; 2h; carrageenin injection) inhibits carrageenin-induced paw oedema in rats (ID50: 2.7 mg/kg). FR167344 (p.o.) inhibits kaolin-induced writhing in mice (ID50: 2.8 mg/kg in 10 min writhing and 4.2 mg/kg in 15 min writhing). FR167344(p.o.) inhibits caerulein-induced pancreatic oedema (ID50: 13.8 mg/kg) and it also increases in amylase and lipase of blood samples (ID50: 10.3 and 7.4 mg/kg, respectively, in rats) [2]. |
分子量 | 673.38 |
分子式 | C30H28BrCl2N5O4 |
CAS No. | 215258-13-2 |
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。
FR167344 free base 215258-13-2 Others FR167344 FR-167344 FR-167344 free base FR 167344 Inhibitor inhibitor inhibit