半岛bd体育手机客户端 说明
一般描述
A cell-permeable triarylpyrrole compound that acts as a selective, non-competitive, high affinity glucagon receptor antagonist (IC50= 3.7 nM, 63 nM, and 60 nM for inhibition of labeled glucagon binding to human, murine, and canine glucagon receptor, respectively). Exhibits diminished antagonistic properties in the presence of Mg2+(by ≥ 20-fold) and exhibits poor affinity for the rat, guinea pig, and rabbit glucagon receptors (IC50>1 ?M). Does not inhibit binding of glucagon-like peptide-1 (GLP-1) to the homologous GLP-1 receptor even at concentrations as high as 10 ?M. Does not affect ligand binding of a panel of other GPCRs and only weakly affects p38 kinase activity (IC50= 1.44 ?M). Potently inhibits glucagon-induced GTPγS binding to Gαs (IC50= 158 nM) and adenylate cyclase activation in hGLUR-CHO cells (Kb= 25 nM). Shown to be orally bioavailable in both mice and rats.
A cell-permeable triarylpyrrole compound that acts as a selective, non-competitive, high affinity glucagon receptor antagonist (IC50= 3.7 nM, 63 nM, and 60 nM for inhibition of labeled glucagon binding to human, murine, and canine glucagon receptor, respectively). Exhibits diminished antagonistic properties in the presence of Mg2+(by ≥20-fold) and exhibits poor affinity for the rat, guinea pig, and rabbit glucagon receptors (IC50>1 ?M). Does not inhibit binding of glucagon-like peptide-1 (GLP-1) to the homologous GLP-1 receptor even at concentrations as high as 10 ?M. Does not affect ligand binding of a panel of other GPCRs and only weakly affects p38 kinase activity (IC50= 1.44 ?M). Potently inhibits glucagon-induced GTPγS binding to Gαs (IC50= 158 nM) and adenylate cyclase activation in hGLUR-CHO cells (Kb= 25 nM). Shown to be orally bioavailable in both mice and rats.
包装
5 mg in Plastic ampoule
Packaged under inert gas
生化/生理作用
Cell permeable: yes
Target IC50: 3.7 nM, 63 nM, and 60 nM for inhibition of labeled glucagon binding to human, murine, and canine glucagon receptor, respectively
Product does not compete with ATP.
Reversible: no
Primary Target
Glucagon Receptor
警告
Toxicity: Standard Handling (A)
重悬
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
其他说明
Dallas-Yang, Q., et al. 2002.Anal. Biochem.301,156.
Cascieri, M.A., et al. 1999.J. Biol. Chem.274,8694.
de Laszlo, S.E., et al. 1999.Bioorg. Med. Chem. Lett.9,641.
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 | C24H20BrClN2O |
| 分子量 | 467.79 |
半岛bd体育手机客户端 性质
| 质量水平 | 100 |
| 测定 | ≥98% (HPLC) |
| 形式 | solid |
| manufacturer/tradename | Calbiochem? |
| 储存条件 | OK to freeze protect from light |
| 颜色 | light beige |
| 溶解性 | DMSO: 45 mg/mL ethanol: 45 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 |
Sigma-Aldrich
m.cnreagent.com
