1. GPCR/G Protein
    Neuronal Signaling
  2. GPR119
  3. GSK1292263

GSK1292263 

Cat. No.: HY-12066 Purity: 99.21%
Handling Instructions

GSK-1292263 is an orally available GPR119 agonist with pEC50s of 6.9 and 6.7 for human and rat GPR119, respectively. GSK-1292263 can be used for the research of type 2 diabetes mellitus (T2DM).

For research use only. We do not sell to patients.

GSK1292263 Chemical Structure

GSK1292263 Chemical Structure

CAS No. : 1032823-75-8

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Solution
10 mM * 1 mL in DMSO USD 99 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 99 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 90 In-stock
Estimated Time of Arrival: December 31
10 mg USD 150 In-stock
Estimated Time of Arrival: December 31
50 mg USD 450 In-stock
Estimated Time of Arrival: December 31
100 mg USD 650 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
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Customer Review

Based on 5 publication(s) in Google Scholar

Top Publications Citing Use of Products

    GSK1292263 purchased from MCE. Usage Cited in: FASEB J. 2016 Jan;30(1):324-35.

    Treatment with 2 synthetic GPR119 agonists, MBX-2982 (MBX) and GSK1292263 (GSK), suppresses T090-induced SREBP-1 expression and mRNA levels of SREBP-1 target genes such as FAS, ACC, and SCD-1.

    GSK1292263 purchased from MCE. Usage Cited in: College of Pharmacy. Seoul National University. 2015 Aug.

    Effects of GPR119 ligands on T090-induced pSREBP-1 and lipogenic enzymes expression. Primary cultured hepatocytes from GPR119-WT and -KO mice and HepG2 cells are pretreated with two GPR119 ligands [(MBX (MBX-2982) or GSK (GSK1292263)] for 30 min and the cells are exposed to T090 for 12 h.
    • Biological Activity

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    • Customer Review

    Description

    GSK-1292263 is an orally available GPR119 agonist with pEC50s of 6.9 and 6.7 for human and rat GPR119, respectively. GSK-1292263 can be used for the research of type 2 diabetes mellitus (T2DM)[1].

    In Vivo

    GSK1292263 upregulates glucagon-like peptide-1 and enhances glucose-dependent insulin secretion and improves glucose homeostasis in type 2 diabetic rats[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: Male neonatal Streptozotocin (STZ)-induced SD rats (7 weeks of age)[2]
    Dosage: 30 mg/kg
    Administration: Orally given; once a day for 2 weeks
    Result: The AUC of plasma glucose (AUCPG) in the single treatment of the GSK1292263 group was numerically lower than that of the vehicle group, but the effect was modest.
    Clinical Trial
    Molecular Weight

    456.56

    Formula

    C₂₃H₂₈N₄O₄S

    CAS No.
    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 20 mg/mL (43.81 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.1903 mL 10.9515 mL 21.9029 mL
    5 mM 0.4381 mL 2.1903 mL 4.3806 mL
    10 mM 0.2190 mL 1.0951 mL 2.1903 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2 mg/mL (4.38 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References

    Purity: 99.71%

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    Product Name:
    GSK1292263
    Cat. No.:
    HY-12066
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