| Identification | Back Directory | [Name]
MBX2982 | [CAS]
1037792-44-1 | [Synonyms]
CS-485
MBX2982
SAR-260093
MBX-2982, >=98%
MBX2982 / MBX-2982
MBX-2982 (SAR260093)
MBX-2982;MBX 2982;MBX2982
2-[1-(5-ethylpyrimidin-2-yl)-4-piperidyl]-4-[[4-(tetrazol-1-yl)phenoxy]methyl]thiazole
pyrimidine, 5-ethyl-2-[4-[4-[[4-(1h-tetrazol-1-yl)phenoxy]methyl]-2-thiazolyl]-1-piperidinyl]-
5-Ethyl-2-[4-[4-[[[4-(1H-tetrazol-1-yl)phenyl]oxy]methyl]thiazol-2-yl]piperidin-1-yl]pyrimidine
5-Ethyl-2-[4-[4-[[[4-(1H-tetrazol-1-yl)phenyl]oxy]methyl]thiazol-2-yl]piperidin-1-yl]pyrimidine MBX-2982 | [Molecular Formula]
C22H24N8OS | [MDL Number]
MFCD22628771 | [MOL File]
1037792-44-1.mol | [Molecular Weight]
448.54 |
| Chemical Properties | Back Directory | [Boiling point ]
683.6±65.0 °C(Predicted) | [density ]
1.42 | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 50 mg/mL (111.47 mM; Need ultrasonic)H2O : < 0.1 mg/mL (insoluble) | [form ]
Powder | [pka]
5.39±0.42(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Description]
MBX-2982 is an agonist of GPR119. It reduces nuclear and total protein levels of sterol regulatory element binding protein 1 (SREBP-1) in HepG2 cells and rat primary hepatocytes under high-glucose and -insulin conditions and increases phosphorylation of the inhibitory form, SREBP-1c. MBX-2982 (10 mg/kg) inhibits hepatic lipid accumulation in wild-type, but not GPR119 knockout, mice fed a high-fat diet. It also increases plasma levels of glucagon-like peptide 1 (GLP-1; ) in mice when administered at a dose of 10 mg/kg prior to, and to a greater extent following, glucose administration. MBX-2982 increases glucokinase activity in an enzyme assay with an EC50 value of 45.11 μM. | [Uses]
MBX-2982 is a selective, orally-available G protein-coupled receptor 119 (GPR119) agonist. | [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 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]. | [References]
[1] Hothersall JD, et al. Sustained wash-resistant receptor activation responses of GPR119 agonists. Eur J Pharmacol. 2015 Sep 5;762:430-42. DOI:10.1016/j.ejphar.2015.06.031
[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. DOI:10.1111/j.1476-5381.2011.01754.x
[3] Yang JW, et al. GPR119: a promising target for nonalcoholic fatty liver disease. FASEB J. 2016 Jan;30(1):324-35. DOI:10.1096/fj.15-273771 |
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