1. GPCR/G Protein
    Neuronal Signaling
  2. GPR119
  3. MBX-2982

MBX-2982 

Cat. No.: HY-15291 Purity: 99.39%
Handling Instructions

MBX-2982 is a selective, orally-available G protein-coupled receptor 119 (GPR119) agonist.

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

MBX-2982 Chemical Structure

MBX-2982 Chemical Structure

CAS No. : 1037792-44-1

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 216 In-stock
Estimated Time of Arrival: December 31
5 mg USD 196 In-stock
Estimated Time of Arrival: December 31
10 mg USD 362 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1164 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 10 publication(s) in Google Scholar

Top Publications Citing Use of Products

    MBX-2982 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.

    MBX-2982 purchased from MCE. Usage Cited in: Patent. US9895370B2.

    When the GPR119 ligand (MBX-2982) is time-dependently treated, AMPK is highly activated (AMPK and ACC phosphorylation).

    MBX-2982 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-2982 or GSK1292263) for 30 min and the cells are exposed to T090 for 12 h.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    MBX-2982 is a selective, orally-available G protein-coupled receptor 119 (GPR119) agonist.

    IC50 & Target

    GPR119[1]

    In Vitro

    In cells pre-treated with MBX-2982 (1 µM) in “chronic incubation/washout” experiments, cAMP accumulation captured by IBMX inclusion is significantly increased compared to control cells (P<0.01; ANOVA; n=3-6) despite extensive washing to remove excess agonist. AR-231,453 produces sustained responses in a similar concentration range to those observed with acute stimulation (a small 1.82 fold shift), with pEC50s of 8.67±0.11 and 8.93±0.17, respectively. Likewise, a large but less severe shift in concentration responses (57.54 fold) is observed for MBX-2982 with respective sustained and acute pEC50s of 7.03±0.13 and 8.79±0.12[1].

    In Vivo

    To examine whether the observations in GLUTag and the primary intestinal cells has physiological relevance, C57BL/6 mice are treated with the GPR119 agonist MBX-2982 at a dose of 10 mg/kg. Note that in order to examine a direct GPR119 effect, no DPP-IV inhibitor is co-administered in this experiment, but a DPP-IV inhibitor is used to preserve active GLP-1 in the blood samples. The plasma GLP-1 levels from the mice dosed with MBX-2982 are increased without a glucose load, indicating that GPR119-mediated GLP-1 secretion is not dependent on glucose[2].

    Clinical Trial
    Molecular Weight

    448.54

    Formula

    C₂₂H₂₄N₈OS

    CAS No.

    1037792-44-1

    SMILES

    CCC1=CN=C(N2CCC(C3=NC(COC4=CC=C(N5N=NN=C5)C=C4)=CS3)CC2)N=C1

    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 : 50 mg/mL (111.47 mM; Need ultrasonic)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.2295 mL 11.1473 mL 22.2946 mL
    5 mM 0.4459 mL 2.2295 mL 4.4589 mL
    10 mM 0.2229 mL 1.1147 mL 2.2295 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: ≥ 2.75 mg/mL (6.13 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    Kinase Assay
    [1]

    HEK-GPR119 cells are transfected with GloSensor 22F plasmid and used for dynamic cAMP measurements 24-30 h later. Cell suspensions are made by dislodging the cells using PBS wash and Accutase treatment followed by resuspension in culture media. Cells are then washed twice by pelleting through centrifugation (300g, 5 min) and resuspension in assay buffer (Hank's Balanced Salt Solution supplemented with 20 mM HEPES and 0.01% fatty acid free BSA, pH 7.4). Cells are then counted and diluted to 600,000 cells/mL in buffer, before GloSensor cAMP reagent is added (2% v/v) and equilibrated with the cells for 2 h at 20°C with periodic mixing. 50 µl/well of cells are added to white-bottomed 384 well plates (30,000 cells/well) in triplicate and baseline luminescence is measuring using an Envision plate-reader. 5 μL of MBX-2982 (serially diluted in DMSO and then diluted 1:100 in assay buffer to obtain ×10 concentrated solution) is manually added to the assay wells to achieve the stated final concentration. Plates are incubated at 20°C with luminescence read at regular intervals to detect dynamic cAMP changes over time within the same wells. cAMP responses at each time-point are expressed as fold over control (vehicle-treated cells)[1].

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

    Cell Assay
    [1]

    HEK-GPR119 cells are grown to confluency in flasks, and cell suspensions are made by dislodging cells using PBS wash and accutase treatment followed by resuspension in culture media. Cells are then washed twice by pelleting through centrifugation (227g, 7 min, 20°C) and resuspension in warm assay buffer (Hank's Balanced Salt Solution supplemented with 20 mM HEPES and 0.01% fatty acid free BSA, pH 7.4), with a 5 min incubation at 37°C after the second wash. Cells are then counted and diluted to 200,000 cells/mL in warm assay buffer[1].

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

    Animal Administration
    [2]

    Mice[2]
    C57BL/6 male mice are used. Overnight fasted, 10 week-old male mice (n=20 per group) are given either vehicle (15% polyethylene glycol 400+85% of 23.5% hydroxypropyl-β-cyclodextrin) or MBX-2982 at 10 mg/kg via oral gavage. Half of the animals (n=10 per group) are killed by CO2 asphyxiation 30 min after compound dosing, and blood is collected by cardiac puncture. To preserve active GLP-1, a DPP-IV inhibitor (10 µL per 1 mL of blood) is pre-added to the blood collection tubes and, before the cardiac puncture, the walls of the syringes are rinsed with the DPP-IV inhibitor. The other half of the animals (n=10 per group) received a bolus of oral glucose (3 g/kg) 30 min after compound dosing, and are killed for blood collection 10 min after the glucose load. GLP-1 levels in the plasma samples are measured using the active GLP-1 (ver 2) kit.

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

    References
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