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首页-小分子抑制剂&激动剂-GPCR-Free Fatty Acid Receptor (FFAR)-BTI-A-404
BTI-A-404

Chemical Structure : BTI-A-404

CAS No.: 537679-57-5

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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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

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.

物理化学性质&存储条件

分子量 378.48
分子式 C22H26N4O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

4-[4-(dimethylamino)phenyl]-N-(3,5-dimethylphenyl)-6-methyl-2-oxo-1,2,3,4-tetrahydro-5-pyrimidinecarboxamide

参考文献

1. Park BO, et al. Eur J Pharmacol. 2016 Jan 15;771:1-9.

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