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    GSK1292263
    GSK1292263

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1804
    CAS #: 1032823-75-8Purity ≥98%

    Description: GSK1292263 is a novel and potent GPR119 (G-protein-coupled receptor 119) agonist which has potential for the treatment of type 2 diabetes. It is currently undergoing phase 2 clinical trial for type 2 diabetes. GSK1292263 improves glucose regulation in animal models of diabetes, but has no effect on plasma glucose in type 2 diabetics. GSK1292263 treatment displayed little inhibition towards CYPs (CYP1A2, 2C9, 2C19, 2D6, 3A4), p-GP, OATP1B3, or OCT2. However, GSK1292263 inhibited BCRP and OATP1B1, which are transporters involved in statin disposition 1.

    References: Eur J Med Chem. 2011 Jul;46(7):2901-7; Xenobiotica. 2013 Jun;43(6):498-508.

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    Molecular Weight (MW)456.56
    FormulaC23H28N4O4S
    CAS No.1032823-75-8
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 34 mg/mL (74.5 mM)
    Water: <1 mg/mL
    Ethanol:<1 mg/mL
    Solubility (In vivo)30% Propylene glycol, 5% Tween 80, 65% D5W: 30 mg/mL 
    SynonymsGSK1292263; GSK 1292263l; GSK-1292263


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    In Vitro

    In vitro activity: GSK1292263 is a novel, potent GPR119 agonist, which showed potential for the treatment of type 2 diabetes. It is currently undergoing phase 2 clinical trial for type 2 diabetes. GSK1292263 improves glucose regulation in animal models of diabetes, but has no effect on plasma glucose in type 2 diabetics. GSK1292263 treatment displayed little inhibition towards CYPs (CYP1A2, 2C9, 2C19, 2D6, 3A4), p-GP, OATP1B3, or OCT2. However, GSK1292263 inhibited BCRP and OATP1B1, which are transporters involved in statin disposition 1.


    Kinase Assay: GSK-1292263 is selected from 1538 compounds by using Hypo1, the Fit-Value and Estimate of GSK-1292263 that is aligned in Hypo1 are 8.8 and 7.7 (nM), respectively


    Cell Assay: In vitro, GSK1292263 treatment displayed little inhibition towards CYPs (CYP1A2, 2C9, 2C19, 2D6, 3A4), p-GP, OATP1B3, or OCT2. However, GSK1292263 inhibited BCRP and OATP1B1, which are transporters involved in statin disposition 1.

    In VivoGSK-1292263 administrated at a single dose of 3-30 mg/kg in the absence of nutrients correlates with increased levels of circulating gastrointestinal peptides, including glucagon-like peptide 1 (GLP-1), gastric inhibitory polypeptide (GIP), peptide YY (PYY) and glucagon in male Sprague-Dawley rats, the increase is enhanced following administration of glucose in the oral glucose tolerance test (OGTT). GSK-129226 significant increases in the peak insulin response and insulin AUC(0-15 min) of 30-60% compared with values in the vehicle control cohort in the intravenous glucose tolerance test in rats, this insulin upregulation correlated with a significant increase in the glucose disposal rate. GSK-1292263 is associated with a statistically significant increase in insulin immunoreactivity in pancreatic sections in a 6-week study performed in Zucker diabetic fatty rats, compared with insulin immunoreactivity in samples obtained from rats receiving vehicle control. GSK-1292263 administrated at dose of 10 or 30 mg/kg or vehicle control at 2 hours prior to insulin infusion in hyperinsulinemic-euglycemic clamps stimulates glucagon secretion without increasing blood glucose levels Sprague-Dawley rats.
    Animal model Rats
    Formulation & Dosage 3-30 mg/kg
    ReferencesEur J Med Chem. 2011 Jul;46(7):2901-7; Xenobiotica. 2013 Jun;43(6):498-508.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

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