CATPB - CAS 1322598-09-3
Category: Inhibitor
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Molecular Formula:
Molecular Weight:
CATPB is a human FFA2 inverse agonist (pKi = 7.87). It increases forskolin-induced cAMP production, and inhibits acetate-induced MAPK signaling in cells expressing human FFA2.
Brife Description:
human FFA2 inverse agonist
≥98% by HPLC
(S)-3-(2-(3-Chlorophenyl)acetamido)-4-(4-(trifluoromethyl)phenyl)butanoic acid
Canonical SMILES:
1.FFAR2-FFAR3 receptor heteromerization modulates short-chain fatty acid sensing.
Ang Z;Xiong D;Wu M;Ding JL FASEB J. 2018 Jan;32(1):289-303. doi: 10.1096/fj.201700252RR. Epub 2017 Sep 7.
Free fatty acid receptors 2 and 3 (FFAR2/FFA2/GPR43 and FFAR3/FFA3/GPR41) are mammalian receptors for gut microbiota-derived short-chain fatty acids (SCFAs). These receptors are promising drug targets for obesity, colitis, colon cancer, asthma, and arthritis. Here, we demonstrate that FFAR2 and FFAR3 interact to form a heteromer in primary human monocytes and macrophages ;via; proximity ligation assay, and during heterologous expression in HEK293 cells ;via; bimolecular fluorescence complementation and fluorescence resonance energy transfer. The FFAR2-FFAR3 heteromer displayed enhanced cytosolic Ca;2+; signaling (1.5-fold increase relative to homomeric FFAR2) and β-arrestin-2 recruitment (30-fold increase relative to homomeric FFAR3). The enhanced heteromer signaling was attenuated by FFAR2 antagonism (CATPB), G;αq; inhibition (YM254890), or G;αi; inhibition (pertussis toxin). Unlike homomeric FFAR2/3, the heteromer lacked the ability to inhibit cAMP production but gained the ability to induce p38 phosphorylation in HEK293 and inflammatory monocytes ;via; a CATPB- and YM254890-sensitive mechanism. Our data, taken together, reveal that FFAR2 and FFAR3 may interact to form a receptor heteromer with signaling that is distinct from the parent homomers-a novel pathway for drug targeting.
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CAS 1322598-09-3 CATPB

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