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

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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10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 68 In-stock
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Customer Review

Based on 5 publication(s) in Google Scholar

GSK1292263 Related Antibodies

Top Publications Citing Use of Products

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

    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 MedChemExpress. 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

    • Purity & Documentation

    • References

    • 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].

    MedChemExpress (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.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    CC(C1=NOC(N2CCC(CC2)COC3=CN=C(C=C3)C4=CC=C(C=C4)S(C)(=O)=O)=N1)C
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 20 mg/mL (43.81 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" 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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
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    Concentration
    ×
    Volume
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    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

    V1

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    C2

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    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    90% Corn Oil

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

      This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.71%

    COA (246 KB) HNMR (187 KB) LCMS (442 KB)

    Handling Instructions (2659 KB)
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.1903 mL 10.9515 mL 21.9029 mL 54.7573 mL
    5 mM 0.4381 mL 2.1903 mL 4.3806 mL 10.9515 mL
    10 mM 0.2190 mL 1.0951 mL 2.1903 mL 5.4757 mL
    15 mM 0.1460 mL 0.7301 mL 1.4602 mL 3.6505 mL
    20 mM 0.1095 mL 0.5476 mL 1.0951 mL 2.7379 mL
    25 mM 0.0876 mL 0.4381 mL 0.8761 mL 2.1903 mL
    30 mM 0.0730 mL 0.3650 mL 0.7301 mL 1.8252 mL
    40 mM 0.0548 mL 0.2738 mL 0.5476 mL 1.3689 mL
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    GSK1292263 Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    GSK12922631032823-75-8GSK 1292263GSK-1292263GPR119G Protein-Coupled Receptor 119type2diabetesmellitusT2DMInhibitorinhibitorinhibit

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