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Glucagon Receptor Antagonist II-CAS 191034-25-0-Calbiochem

品牌
Sigma-Aldrich
CAS
191034-25-0
货号
346003
规格纯度
The Glucagon Receptor Antagonist II, also referenced under CAS 191034-25-0, controls the biological activity of Glucagon Receptor.
参考价格
2741.8 *本价格含增值税费
促销
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数量
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产品名称:
191034-25-0
Glucagon Receptor Antagonist II-CAS 191034-25-0-Calbiochem
2-(4-Pyridyl)-5-(4-chlorophenyl)-3-(5-bromo-2-propyloxyphenyl)pyrrole, L-168,049
产品介绍:

产品说明

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 µM). Does not inhibit binding of glucagon-like peptide-1 (GLP-1) to the homologous GLP-1 receptor even at concentrations as high as 10 µM. Does not affect ligand binding of a panel of other GPCRs and only weakly affects p38 kinase activity (IC50 = 1.44 µM). 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 µM). Does not inhibit binding of glucagon-like peptide-1 (GLP-1) to the homologous GLP-1 receptor even at concentrations as high as 10 µM. Does not affect ligand binding of a panel of other GPCRs and only weakly affects p38 kinase activity (IC50 = 1.44 µM). 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

产品性质

质量水平100
测定≥98% (HPLC)
形式solid
manufacturer/tradenameCalbiochem®
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
WGKWGK 1
闪点(F)Not applicable
闪点(C)Not applicable

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