MBX-2982
Based on 13 publication(s) in Google Scholar
MBX-2982 is a selective, orally-available G protein-coupled receptor 119 (GPR119) agonist.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.68%
- CAS 番号: 1037792-44-1
- 分子式: C22H24N8OS
- 分子量:448.54
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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MedChemExpress（MCE）の使用を引用している文献 MBX-2982
More- Nat Commun. 2022 Nov 17;13(1):7033. [Abstract]
- J Exp Clin Cancer Res. 2018 Nov 29;37(1):295. [Abstract]
- Cell Commun Signal. 2019 May 23;17(1):49 [Abstract]
- Biochem Pharmacol. 2025 Jul 3:241:117095. [Abstract]
- Cell Prolif. 2025 Mar;58(3):e13764. [Abstract]
- Invest Ophthalmol Vis Sci. 2017 Jun 1;58(7):2930-2938. [Abstract]
- Structure. 2024 Dec 5;32(12):2206-2219.e4. [Abstract]
- FASEB J. 2016 Jan;30(1):324-35. [Abstract]
- Toxicol Appl Pharmacol. 2024 May:486:116945. [Abstract]
- Biomol Ther (Seoul). 2026 May 1;34(3):666-675. [Abstract]
- Patent. US9895370B2.
- Patent. US20170143714A1.
- College of Pharmacy. Seoul National University. 2015 Aug.
Customer Validation & Images
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生物活性
GPR119[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
0.005 mM
Compound: 4, MBX-2982
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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
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[PMID: 24751443] |
| CHO-K1 | IC50 |
>100 μM
Compound: 1; MBX-2982
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Cytotoxicity against CHOK1 cells
Cytotoxicity against CHOK1 cells
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[PMID: 29103971] |
| HFL1 | IC50 |
>100 μM
Compound: 1; MBX-2982
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Cytotoxicity against HFL1 cells
Cytotoxicity against HFL1 cells
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[PMID: 29103971] |
| L929 | IC50 |
>100 μM
Compound: 1; MBX-2982
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Cytotoxicity against mouse L929 cells
Cytotoxicity against mouse L929 cells
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[PMID: 29103971] |
| NIH3T3 | IC50 |
>100 μM
Compound: 1; MBX-2982
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Cytotoxicity against mouse NIH/3T3 cells
Cytotoxicity against mouse NIH/3T3 cells
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[PMID: 29103971] |
| Vero | IC50 |
>100 μM
Compound: 1; MBX-2982
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Cytotoxicity against African green monkey Vero cells
Cytotoxicity against African green monkey Vero cells
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[PMID: 29103971] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 1037792-44-1
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性状 Solid
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分子量 448.54
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分子式 C22H24N8OS
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Color White to off-white
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SMILES
CCC1=CN=C(N2CCC(C3=NC(COC4=CC=C(N5N=NN=C5)C=C4)=CS3)CC2)N=C1
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (13)
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Journal Impact Factor
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Most Recent
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Nat Commun
2022 Nov 17;13(1):7033. PMID: 36396650 -
J Exp Clin Cancer Res
GPR119 agonist enhances gefitinib responsiveness through lactate-mediated inhibition of autophagy. [Abstract]2018 Nov 29;37(1):295. PMID: 30497501 -
Cell Commun Signal
A piggyBac-based TANGO GFP assay for high throughput screening of GPCR ligands in live cells. [Abstract]2019 May 23;17(1):49 PMID: 31122241 -
Biochem Pharmacol
The C-terminal region regulates the constitutive signaling activity of GPR119: G protein recruitment. [Abstract]2025 Jul 3:241:117095. PMID: 40617490 -
Cell Prolif
Terazosin, a repurposed GPR119 agonist, ameliorates mitophagy and β-cell function in NAFPD by inhibiting MST1-Foxo3a signalling pathway. [Abstract]2025 Mar;58(3):e13764. PMID: 39413003 -
Invest Ophthalmol Vis Sci
A GPR119 Signaling System in the Murine Eye Regulates Intraocular Pressure in a Sex-Dependent Manner. [Abstract]2017 Jun 1;58(7):2930-2938. PMID: 28593245 -
Structure
Native mass spectrometry prescreening of G protein-coupled receptor complexes for cryo-EM structure determination. [Abstract]2024 Dec 5;32(12):2206-2219.e4. PMID: 39471802 -
FASEB J
2016 Jan;30(1):324-35. PMID: 26399788
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.
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Toxicol Appl Pharmacol
In silico and in vitro assessment of drugs potentially causing adverse effects by inhibiting CYP17A1. [Abstract]2024 May:486:116945. PMID: 38688424 -
Biomol Ther (Seoul)
2026 May 1;34(3):666-675. PMID: 42059036 -
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).
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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.
溶剤 & 溶解度
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)
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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.
Please enter the basic information of animal experiments:
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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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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
プロトコル
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) has not independently confirmed the accuracy of these methods. They are for reference only.
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) has not independently confirmed the accuracy of these methods. They are for reference only.
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) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
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データシート (278 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Hothersall JD, et al. Sustained wash-resistant receptor activation responses of GPR119 agonists. Eur J Pharmacol. 2015 Sep 5;762:430-42. [Content Brief]
[2]. Lan H, et al. Agonists at GPR119 mediate secretion of GLP-1 from mouse enteroendocrine cells through glucose-independent pathways. Br J Pharmacol. 2012 Apr;165(8):2799-807. [Content Brief]
[3]. Yang JW, et al. GPR119: a promising target for nonalcoholic fatty liver disease. FASEB J. 2016 Jan;30(1):324-35. [Content Brief]
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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