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508941 GPR40 Agonist III - CAS 1206628-99-0 - Calbiochem

A cell-permeable, highly potent, and selective agonist of free fatty acid receptor 1 (FFA1; GPR40; EC₅₀ = 20 nM in FFA1-transfected HEK-293 cells).

FDS (Fiches de données de sécurité), certificats d’analyse (CoA) et de qualité (CoQ), dossiers, brochures et autres documents disponibles.

Synonymes: FFA1 Agonist III, Free Fatty Acid Receptor 1 Agonist III

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508941
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Tableau de caractéristiques principal

CAS #Empirical Formula
1206628-99-0C₁₉H₁₅NO₂

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      Description
      OverviewA cell-permeable, orally bioavailable, non-toxic, alkyne derivative that acts as a highly potent, and selective agonist of free fatty acid receptor 1 (FFA1; GPR40; EC50 = 20 nM in FFA1-transfected HEK-293 cells). Exhibits lower lipophilicity and excellent metabolic stability. Demonstrates over 100-fold greater selectivity over GPR43, GPR41, GPR120, PPARγ and 55 other receptors, transporters, and enzymes. Improves glucose tolerance in type 2 diabetic mice (~50 mg/kg) with efficacy comparable to DPPIV inhibitor, sitagliptin (~10 mg/kg). Displays favorable pharmacokinetic properties with t 1/2= 17 min and Cmax of 5071 (ng/ml).

      Please note that the molecular weight for this compound is batch-specific due to variable water content.
      Catalogue Number508941
      Brand Family Calbiochem®
      SynonymsFFA1 Agonist III, Free Fatty Acid Receptor 1 Agonist III
      References
      ReferencesChristiansen, E., et al. 2013. J. Med. Chem. 56, 982.
      Product Information
      CAS number1206628-99-0
      FormOff-white powder
      Hill FormulaC₁₉H₁₅NO₂
      Chemical formulaC₁₉H₁₅NO₂
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Purity≥98% by HPLC
      Physicochemical Information
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
      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 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Référence GTIN
      5089410001 04055977261448

      Documentation

      GPR40 Agonist III - CAS 1206628-99-0 - Calbiochem FDS

      Titre

      Fiche de données de sécurité des matériaux (FDS) 

      Références bibliographiques

      Aperçu de la référence bibliographique
      Christiansen, E., et al. 2013. J. Med. Chem. 56, 982.
      Fiche technique

      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.

      Revision07-March-2014 JSW
      SynonymsFFA1 Agonist III, Free Fatty Acid Receptor 1 Agonist III
      DescriptionA cell-permeable, orally bioavailable, non-toxic, alkyne derivative that acts as a highly potent, and selective agonist of free fatty acid receptor 1 (FFA1; GPR40; EC50 = 20 nM in FFA1-transfected HEK-293 cells). Exhibits lower lipophilicity and excellent metabolic stability. Demonstrates over 100-fold greater selectivity over GPR43, GPR41, GPR120, PPARγ and 55 other receptors, transporters, and enzymes. Improves glucose tolerance in type 2 diabetic mice (~50 mg/kg) with efficacy comparable to DPPIV inhibitor, sitagliptin (~10 mg/kg). Displays favorable pharmacokinetic properties with t 1/2= 17 min and Cmax of 5071 (ng/ml).
      FormOff-white powder
      Intert gas (Yes/No) Packaged under inert gas
      CAS number1206628-99-0
      Chemical formulaC₁₉H₁₅NO₂
      Structure formulaStructure formula
      Purity≥98% by HPLC
      SolubilityDMSO (100 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 3 months at -20°C.
      Toxicity Standard Handling
      ReferencesChristiansen, E., et al. 2013. J. Med. Chem. 56, 982.