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346003 Glucagon Receptor Antagonist II - CAS 191034-25-0 - Calbiochem

346003
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Overview

Replacement Information

Key Spec Table

Empirical FormulaCAS #
C₂₄H₂₀BrClN₂O191034-25-0

Products

Catalogue NumberPackaging Qty/Pack
346003-5MG Plastic ampoule 5 mg
Description
OverviewA 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.
Catalogue Number346003
Brand Family Calbiochem®
Synonyms2-(4-Pyridyl)-5-(4-chlorophenyl)-3-(5-bromo-2-propyloxyphenyl)pyrrole, L-168,049
References
ReferencesDallas-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.
Product Information
CAS number191034-25-0
ATP CompetitiveN
FormLight beige solid
Hill FormulaC₂₄H₂₀BrClN₂O
Chemical formulaC₂₄H₂₀BrClN₂O
ReversibleN
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Primary TargetGlucagon Receptor
Primary Target IC<sub>50</sub>3.7 nM, 63 nM, and 60 nM for inhibition of labeled glucagon binding to human, murine, and canine glucagon receptor, respectively
Purity≥98% by HPLC
Physicochemical Information
Cell permeableY
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Standard Handling
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications

Documentation

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

Title

Safety Data Sheet (SDS) 

Glucagon Receptor Antagonist II - CAS 191034-25-0 - Calbiochem Certificates of Analysis

TitleLot Number
346003

References

Reference overview
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.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision08-April-2011 RFH
Synonyms2-(4-Pyridyl)-5-(4-chlorophenyl)-3-(5-bromo-2-propyloxyphenyl)pyrrole, L-168,049
DescriptionA 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.
FormLight beige solid
Intert gas (Yes/No) Packaged under inert gas
CAS number191034-25-0
Chemical formulaC₂₄H₂₀BrClN₂O
Structure formulaStructure formula
Purity≥98% by HPLC
SolubilityDMSO (45 mg/ml) or Ethanol (45 mg/ml)
Storage +2°C to +8°C
Protect from light
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Toxicity Standard Handling
ReferencesDallas-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.