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533640 GPR119 Agonist II, GSK1292263 - CAS 1032823-75-8 - Calbiochem

GPR119 Agonist II, GSK1292263, CAS 1032823-75-8, is a potent, selective, and reversible agonist of GPR119 (pEC50 ~ 6.8 for human, mouse & rat GPR119). Stimulates glucose-dependent insulin secretion.

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

Synonyms: 5-(((1-(3-(1-Methylethyl)-1,2,4-oxadiazol-5-yl)-4-piperidinyl)methyl)oxy]-2-(4-(methylsulfonyl)phenyl)pyridine, GSK-1292263

Primary Target: GPR119
533640
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Overview

Replacement Information

Key Specifications Table

CAS #Empirical Formula
1032823-75-8C₂₃H₂₈N₄O₄S

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      Description
      OverviewAn orally bioavailable, non-toxic oxadiazolyl-piperidinylpyridine compound that acts as a potent, selective and reversible agonist of GPR119 (pEC50 ~ 6.8 for hGPR119 & rat GPR119) with no significant in vitro off-target effects in 102 assays (in the range of 1 - 10 µM) and against CYPs (CYP1A2, 2C9, 2C19, 2D6, 3A4), Pgp, OATP1B3, or OCT2 (IC50 > 30 µM). Stimulates glucose-dependent/sensitive insulin secretion (pEC50 = 8.5 in GLUTag cells), improves glucose tolerance, elevates circulating GIP (glucose-dependent insulinotropic peptide) & GLP-1 (glucagon like peptide-1) levels and reduces body weight and food intake in rats. Also functions as a lipid modifying agent by increasing fasting plasma high density lipoprotein cholesterol (HDLc) and reducing fasting LDLc, as well as fasting and prandial triglycerides.

      Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
      Catalogue Number533640
      Brand Family Calbiochem®
      Synonyms5-(((1-(3-(1-Methylethyl)-1,2,4-oxadiazol-5-yl)-4-piperidinyl)methyl)oxy]-2-(4-(methylsulfonyl)phenyl)pyridine, GSK-1292263
      References
      ReferencesNunez, D.J., et al. 2014. PLoS ONE. 9, e92494.
      Polli, J.W., et al. 2013. Xenobiotica. 43, 498.
      Product Information
      CAS number1032823-75-8
      FormWhite solid
      Hill FormulaC₂₃H₂₈N₄O₄S
      Chemical formulaC₂₃H₂₈N₄O₄S
      ReversibleY
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetGPR119
      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 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Identification Number
      Catalog Number GTIN
      5.33640.00014055977286557

      Documentation

      GPR119 Agonist II, GSK1292263 - CAS 1032823-75-8 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Nunez, D.J., et al. 2014. PLoS ONE. 9, e92494.
      Polli, J.W., et al. 2013. Xenobiotica. 43, 498.
      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.

      Revision20-November-2015 JSW
      Synonyms5-(((1-(3-(1-Methylethyl)-1,2,4-oxadiazol-5-yl)-4-piperidinyl)methyl)oxy]-2-(4-(methylsulfonyl)phenyl)pyridine, GSK-1292263
      DescriptionAn orally bioavailable, non-toxic oxadiazolyl-piperidinylpyridine compound that acts as a potent, selective and reversible agonist of GPR119 (pEC50 ~ 6.8 for hGPR119 & rat GPR119) with no significant in vitro off-target effects in 102 assays (in the range of 1 - 10 µM) and against CYPs (CYP1A2, 2C9, 2C19, 2D6, 3A4), Pgp, OATP1B3, or OCT2 (IC50 > 30 µM). Stimulates glucose-dependent/sensitive insulin secretion (pEC50 = 8.5 in GLUTag cells), improves glucose tolerance, elevates circulating GIP (glucose-dependent insulinotropic peptide) & GLP-1 (glucagon like peptide-1) levels and reduces body weight and food intake in rats. Also functions as a lipid modifying agent by increasing fasting plasma high density lipoprotein cholesterol (HDLc) and reducing fasting LDLc, as well as fasting and prandial triglycerides.
      FormWhite solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number1032823-75-8
      Chemical formulaC₂₃H₂₈N₄O₄S
      Purity≥98% by HPLC
      SolubilityDMSO (50 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
      ReferencesNunez, D.J., et al. 2014. PLoS ONE. 9, e92494.
      Polli, J.W., et al. 2013. Xenobiotica. 43, 498.