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

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

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CAS 番号 : 1037792-44-1

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10 mM * 1 mL in DMSO
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 USD 148 在庫あり
Solution
10 mM * 1 mL in DMSO USD 148 在庫あり
Solid
5 mg $135 在庫あり
10 mg $228 在庫あり
25 mg $410 在庫あり
50 mg $620 在庫あり
100 mg $930 在庫あり
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カスタマーレビュー

Based on 12 publication(s) in Google Scholar

Other Forms of MBX-2982:

MBX-2982 関連抗体

Top Publications Citing Use of Products

    MBX-2982 purchased from MedChemExpress. 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 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.

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

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    • 純度とドキュメンテーション

    • 参考文献

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    製品説明

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

    IC50 & Target

    GPR119[1]

    Cellular Effect
    Cell Line Type Value Description References
    CHO EC50
    0.005 mM
    Compound: 4, MBX-2982
    Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
    Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
    		[PMID: 24751443]
    CHO-K1 IC50
    >100 μM
    Compound: 1; MBX-2982
    Cytotoxicity against CHOK1 cells
    Cytotoxicity against CHOK1 cells
    		[PMID: 29103971]
    HFL1 IC50
    >100 μM
    Compound: 1; MBX-2982
    Cytotoxicity against HFL1 cells
    Cytotoxicity against HFL1 cells
    		[PMID: 29103971]
    L929 IC50
    >100 μM
    Compound: 1; MBX-2982
    Cytotoxicity against mouse L929 cells
    Cytotoxicity against mouse L929 cells
    		[PMID: 29103971]
    NIH3T3 IC50
    >100 μM
    Compound: 1; MBX-2982
    Cytotoxicity against mouse NIH/3T3 cells
    Cytotoxicity against mouse NIH/3T3 cells
    		[PMID: 29103971]
    Vero IC50
    >100 μM
    Compound: 1; MBX-2982
    Cytotoxicity against African green monkey Vero cells
    Cytotoxicity against African green monkey Vero cells
    		[PMID: 29103971]
    体外実験

    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].

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

    MBX-2982 関連抗体
    体内実験

    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].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    臨床実験
    分子量

    448.54

    分子式

    C22H24N8OS
    CAS 番号
    Appearance

    Solid

    Color

    White to off-white

    SMILES

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

    Room temperature in continental US; may vary elsewhere.
    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : 50 mg/mL (111.47 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    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
    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.

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    体内:

    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: ≥ 2.75 mg/mL (6.13 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.75 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 (27.5 mg/mL) to 900 μL Corn oil, and mix evenly.

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

    Dosage

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
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    +
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    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.
    純度とドキュメンテーション
    参考文献
    キナーゼ実験
    [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].

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    細胞実験
    [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].

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    動物実験
    [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.

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    参考文献

    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 2.2295 mL 11.1473 mL 22.2946 mL 55.7364 mL
    5 mM 0.4459 mL 2.2295 mL 4.4589 mL 11.1473 mL
    10 mM 0.2229 mL 1.1147 mL 2.2295 mL 5.5736 mL
    15 mM 0.1486 mL 0.7432 mL 1.4863 mL 3.7158 mL
    20 mM 0.1115 mL 0.5574 mL 1.1147 mL 2.7868 mL
    25 mM 0.0892 mL 0.4459 mL 0.8918 mL 2.2295 mL
    30 mM 0.0743 mL 0.3716 mL 0.7432 mL 1.8579 mL
    40 mM 0.0557 mL 0.2787 mL 0.5574 mL 1.3934 mL
    50 mM 0.0446 mL 0.2229 mL 0.4459 mL 1.1147 mL
    60 mM 0.0372 mL 0.1858 mL 0.3716 mL 0.9289 mL
    80 mM 0.0279 mL 0.1393 mL 0.2787 mL 0.6967 mL
    100 mM 0.0223 mL 0.1115 mL 0.2229 mL 0.5574 mL
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    MBX-2982 Related Classifications

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    一般には略語で表示されます：C1V1 = C2V2

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      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:

    MBX-29821037792-44-1MBX2982MBX 2982GPR119G Protein-Coupled Receptor 119Inhibitorinhibitorinhibit

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    製品番号:
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