346003

Sigma-Aldrich

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

The Glucagon Receptor Antagonist II, also referenced under CAS 191034-25-0, controls the biological activity of Glucagon Receptor.

Sinónimos:
Glucagon Receptor Antagonist II - CAS 191034-25-0 - Calbiochem, 2-(4-Pyridyl)-5-(4-chlorophenyl)-3-(5-bromo-2-propyloxyphenyl)pyrrole, L-168,049
Empirical Formula (Hill Notation):
C24H20BrClN2O
Número de CAS:
Peso molecular:
467.79

storage conditions

+2C to +8C

Nivel de calidad

100

ensayo

≥98% (HPLC)

formulario

solid

manufacturer/tradename

Calbiochem®

condiciones de almacenamiento

OK to freeze
protect from light

color

light beige

solubilidad

DMSO: 45 mg/mL
ethanol: 45 mg/mL

enviado en

ambient

Descripción general

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.

Envase

5 mg in Plastic ampoule
Packaged under inert gas

Acciones bioquímicas o fisiológicas

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

Advertencia

Toxicity: Standard Handling (A)

Reconstitución

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Otras notas

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.

Información legal

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

WGK Alemania

WGK 1

Punto de inflamabilidad F

Not applicable

Punto de inflamabilidad C

Not applicable

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