MBX-2982

SKU: orb1307432

Description

MBX-2982

Research Area

Metabolism Research, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1037792-44-1
• MW: 448.54
• Purity: 98.83%
• Formula: C₂₂H₂₄N₈OS
• SMILES: CCc1cnc(nc1)N1CCC(CC1)c1ncc(COc2ccc(cc2)-n2cnnn2)s1
• Target: GPCR
• Solubility: DMSO:50 mg/mL (111.47 mM);10% DMSO+90% Corn Oil:2.5 mg/mL (5.57 mM)

Bioactivity

• In Vivo:
  To determine the physiological relevance of findings in GLUTag and primary intestinal cells, C57BL/6 mice were administered 10 mg/kg of the GPR119 agonist MBX-2982, without co-administration of a DPP-IV inhibitor, to assess the direct effects of GPR119 activation. However, a DPP-IV inhibitor was utilized to maintain active GLP-1 levels in blood samples. Results showed elevated plasma GLP-1 levels in mice treated with MBX-2982, even in the absence of a glucose load, demonstrating that GPR119-induced GLP-1 secretion does not require glucose (2).
• In Vitro:
  In cells that underwent chronic incubation and subsequent washout with MBX-2982 (1 μM), a significant rise in cAMP levels was observed, as measured by IBMX inclusion, when compared to control cells, indicating enhanced accumulation despite thorough washing to eliminate any excess agonist (P<0.01; ANOVA; n=3-6). Similarly, AR-231,453 elicited prolonged responses within a comparable concentration range to acute exposure, showing a modest increase in potency (1.82-fold difference), with pEC50 values of 8.67±0.11 for sustained exposure and 8.93±0.17 for acute. Furthermore, MBX-2982 displayed a substantial yet smaller alteration in concentration response curves during sustained versus acute exposure (57.54-fold difference), with pEC50 values of 7.03±0.13 for sustained and 8.79±0.12 for acute treatment.
• Cell Research:
  MBX-2982 is serially diluted in DMSO and then diluted 1:100 in assay buffer to obtain ×10 concentrated solutionis. 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

MBX2982, MBX-2982, MBX 2982, G Protein-Coupled Receptor 119, GPR119, inhibit, Inhibitor

Compound Identifiers

PubChem CID

46200973