MBX2982

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

MBX-2982 是一种选择性口服 GPR119 激动剂，用于治疗 2 型糖尿病。

MBX-2982 is a selective, orally-available GPR119 agonist for the treatment of type 2 tiabetes.(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.(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.

——

——

MBX-2982 | MBX 2982 | MBX2982 | SAR-260093

Cell Cycle/DNA Damage

GPR

GPR119

Metabolic Disease

——

1037792-44-1

448.54

C22H24N8OS

>98% (HPLC)

DMSO: 10 mM

CCC1=CN=C(N2CCC(C3=NC(COC4=CC=C(N5N=NN=C5)C=C4)=CS3)CC2)N=C1

4-((4-(1H-tetrazol-1-yl)phenoxy)methyl)-2-(1-(5-ethylpyrimidin-2-yl)piperidin-4-yl)thiazole

(-20℃)

With Ice Pack

≥ 2 years