Chemical Structure : BTI-A-404
货号: PC-24797Not For Human Use, Lab Use Only.
BTI-A-404 is a selective and potent competitive inverse agonist / antagonist of human GPR43 (FFA2R) with cAMP IC50 of 9.5 uM.
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BTI-A-404 is a selective and potent competitive inverse agonist / antagonist of human GPR43 (FFA2R) with cAMP IC50 of 9.5 uM.
BTI-A-404 increased intracellular level of cAMP (IC50=9.5 uM) and reversed the effect of propionate on cAMP production only in the presence of hGPR43 in Glosensor cell line, but not in Glosensor cells without hGPR43.
BTI-A-404 is still able to increase cAMP with both of IC50 of 2.1 μM only in the GPR43-overexpressing cells.
BTI-A-404 is inactive against hGPR41 and hChemR23 at concentrations up to 50 μM, also does not inhibits mGPR43.
BTI-A-404 significantly induced the secretion of GLP-1 in NCI-H716 cells.
分子量 | 378.48 | |
分子式 | C22H26N4O2 | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
1. Park BO, et al. Eur J Pharmacol. 2016 Jan 15;771:1-9.
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