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346003 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.

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: 2-(4-Pyridyl)-5-(4-chlorophenyl)-3-(5-bromo-2-propyloxyphenyl)pyrrole, L-168,049

Primary Target: Glucagon Receptor
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346003
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
191034-25-0C₂₄H₂₀BrClN₂O

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      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
      Global Trade Item Number
      Catalogue Number GTIN
      346003-5MG 04055977214598

      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 Protect from light
      +2°C to +8°C
      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.