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MBX-2982

Catalog No. T1793   CAS 1037792-44-1

MBX-2982 is a selective, orally-available GPR119 agonist, used for the treatment of diabetes.

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MBX-2982 Chemical Structure
MBX-2982, CAS 1037792-44-1
Pack Size Availability Price/USD Quantity
1 mg In stock $ 46.00
2 mg In stock $ 66.00
5 mg In stock $ 109.00
10 mg In stock $ 187.00
25 mg In stock $ 365.00
50 mg In stock $ 559.00
100 mg In stock $ 786.00
1 mL * 10 mM (in DMSO) In stock $ 119.00
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Purity: 99.96%
Purity: 98.83%
Purity: 98%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description MBX-2982 is a selective, orally-available GPR119 agonist, used for the treatment of diabetes.
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. In addition, 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 no DPP-IV inhibitor is co-administered in this experiment to examine a direct GPR119 effect, however, 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].
Kinase Assay 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 (300 g, 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].
Cell Research MBX-2982 is serially diluted in DMSO and then diluted 1:100 in assay buffer to obtain ×10 concentrated solutionis[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 (227 g, 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].
Molecular Weight 448.54
Formula C22H24N8OS
CAS No. 1037792-44-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (111.47 mM)

TargetMolReferences and Literature

1. Hothersall JD, et al. Sustained wash-resistant receptor activation responses of GPR119 agonists. Eur J Pharmacol. 2015 Sep 5;762:430-42. 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.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Bioactive Compounds Library Max Neuronal Signaling Compound Library GPCR Compound Library Drug Repurposing Compound Library Anti-Diabetic Compound Library Endocrinology-Hormone Compound Library Bioactive Compound Library ReFRAME Related Library

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Keywords

MBX-2982 1037792-44-1 Endocrinology/Hormones GPCR/G Protein GPR Inhibitor G Protein-Coupled Receptor 119 MBX 2982 GPR119 MBX2982 inhibit inhibitor

 

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