For research use only. Not for therapeutic Use.
MBX-2982 is a selective, orally-available G protein-coupled receptor 119 (GPR119) agonist.
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].
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].
| Catalog Number | I000225 |
| CAS Number | 1037792-44-1 |
| Synonyms | 2-[1-(5-ethylpyrimidin-2-yl)piperidin-4-yl]-4-[[4-(tetrazol-1-yl)phenoxy]methyl]-1,3-thiazole |
| Molecular Formula | C22H24N8OS |
| Purity | ≥95% |
| InChI | InChI=1S/C22H24N8OS/c1-2-16-11-23-22(24-12-16)29-9-7-17(8-10-29)21-26-18(14-32-21)13-31-20-5-3-19(4-6-20)30-15-25-27-28-30/h3-6,11-12,14-15,17H,2,7-10,13H2,1H3 |
| InChIKey | NFTMKHWBOINJGM-UHFFFAOYSA-N |
| SMILES | CCC1=CN=C(N=C1)N2CCC(CC2)C3=NC(=CS3)COC4=CC=C(C=C4)N5C=NN=N5 |
| Reference | [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. [3]. Yang JW, et al. GPR119: a promising target for nonalcoholic fatty liver disease. FASEB J. 2016 Jan;30(1):324-35. |
