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

346003
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₂₄H₂₀BrClN₂O 191034-25-0

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      346003-5MG
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          Plastic ampoule 5 mg
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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
          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

          SDS

          Title

          Safety Data Sheet (SDS) 

          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.

          Brochure

          Title
          Calbiochem Biologics 32.2
          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.