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346003

Sigma-Aldrich

Glucagon Receptor Antagonist II

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

Synonym(s):

Glucagon Receptor Antagonist II, 2-(4-Pyridyl)-5-(4-chlorophenyl)-3-(5-bromo-2-propyloxyphenyl)pyrrole, L-168,049

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About This Item

Empirical Formula (Hill Notation):
C24H20BrClN2O
CAS Number:
Molecular Weight:
467.79
UNSPSC Code:
12352200
NACRES:
NA.77

Quality Level

assay

≥98% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

light beige

solubility

DMSO: 45 mg/mL
ethanol: 45 mg/mL

shipped in

ambient

storage temp.

2-8°C

InChI

1S/C24H20BrClN2O/c1-2-13-29-23-8-5-18(25)14-20(23)21-15-22(16-3-6-19(26)7-4-16)28-24(21)17-9-11-27-12-10-17/h3-12,14-15,28H,2,13H2,1H3

InChI key

HHBOWXZOLYQFNY-UHFFFAOYSA-N

General description

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.

Biochem/physiol Actions

Cell permeable: yes
Primary Target
Glucagon Receptor
Product does not compete with ATP.
Reversible: no
Target IC50: 3.7 nM, 63 nM, and 60 nM for inhibition of labeled glucagon binding to human, murine, and canine glucagon receptor, respectively

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Other Notes

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.

Legal Information

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

Storage Class

11 - Combustible Solids

wgk_germany

WGK 1

flash_point_f

Not applicable

flash_point_c

Not applicable


Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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