产品说明
一般描述
A potent, specific, and orally active C5a receptor antagonist. Shown to inhibit the binding of 125I-rhC5a to human neutrophils with a Ki of 2.2 nM, as well as C5a-induced intracellular Ca2+-mobilization, chemotaxis and reactive oxygen species (ROS) generation (IC50 = 3.1 nM, 2.7 nM and 1.6 nM, respectively) with no agonist activity up to 10 µM. Shown to prevent C5a-induced neutrophenia in gerbils (100 µg/kg i.v. or 3-30 mg/kg orally).
A tetrahydronaphthalenyl carboxamide compound that acts as a potent, specific and orally active C5a receptor antagonist. Shown to inhibit the binding of 125I-rhC5a to human neutrophils with a Ki of 2.2 nM, as well as C5a-induced intracellular Ca2+-mobilization, chemotaxis and reactive oxygen species (ROS) generation (IC50 = 3.1 nM, 2.7 nM and 1.6 nM, respectively) with no agonist activity up to 10 µM. Shown to prevent C5a-induced neutrophenia in gerbils (100 µg/kg i.v. or 3-30 mg/kg orally).
包装
1, 5 mg in Plastic ampoule
Packaged under inert gas
生化/生理作用
Target IC50: 3.1 nM, 2.7 nM and 1.6 nM against C5a-induced intracellular Ca2+-mobilization, chemotaxis and reactive oxygen species (ROS) generation, respectively
Primary Target
C5a Receptor
Product does not compete with ATP.
Target Ki: 2.2 nM against the binding of 125I-rhC5a to human neutrophils
Reversible: no
Cell permeable: no
警告
Toxicity: Standard Handling (A)
重悬
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
其他说明
Sumichika, H., et al. 2002. J. Biol. Chem.277, 49403.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
基本信息
经验(实验)分子式 | C30H36N2O2 · xHCl |
分子量 | 456.62 (free base basis) |
产品性质
质量水平 | 100 |
测定 | ≥95% (HPLC) |
形式 | solid |
manufacturer/tradename | Calbiochem® |
储存条件 | OK to freeze desiccated (hygroscopic) protect from light |
颜色 | white |
溶解性 | DMSO: 50 mg/mL methanol: 50 mg/mL |
运输 | ambient |
储存温度 | 2-8℃ |
安全信息
储存分类代码 | 11 - Combustible Solids |
WGK | WGK 1 |
闪点(F) | Not applicable |
闪点(C) | Not applicable |