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MBX-2982

CAS No. : 1037792-44-1

MCE 站：MBX-2982

产品活性：MBX-2982 是一种口服选择性的 G 蛋白偶联受体 119 (GPR119) 激动剂。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：GPR119

In Vitro: In cells pre-treated with MBX-2982 (1 ?M) 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.

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