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MBX-2982

  Cat. No.:  DC7193   Featured
Chemical Structure
1037792-44-1
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More than 5000 active chemicals with high quality for research!
Field of application
MBX-2982 is a selective, orally-available GPR119 agonist for the treatment of type 2 tiabetes.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 1037792-44-1
Chemical Name: MBX 2982
Synonyms: MBX 2982;5-Ethyl-2-[4-[4-[[[4-(1H-tetrazol-1-yl)phenyl]oxy]methyl]thiazol-2-yl]piperidin-1-yl]pyrimidine;MBX-2982;2-[1-(5-Ethylpyrimidin-2-yl)-4-piperidyl]-4-[[4-(tetrazol-1-yl)phenoxy]methyl]thiazole;2-[1-(5-ethylpyrimidin-2-yl)piperidin-4-yl]-4-[[4-(tetrazol-1-yl)phenoxy]methyl]-1,3-thiazole;CS-0745;UNII-B5TRY67L51;SAR-260093;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 MBX-2982
SMILES: CCC1=CN=C(N=C1)N2CCC(CC2)C3=NC(COC4=CC=C(C=C4)N5N=NN=C5)=CS3
Formula: C22H24N8Os
M.Wt: 448.54396
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: 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].
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. 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].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
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