For research use only. Not for therapeutic Use.
AH-7614 is a potent and selective FFA4 (GPR120) antagonist, with pIC50s of 7.1, 8.1, and 8.1 for human, mouse, and rat FFA4, respectively. AH-7614 has selectivity for FFA4 over FFA1 (pIC50<4.6). AH-7614 is able to block effects of both the polyunsaturated ω-6 fatty acid linoleic acid and the synthetic FFA4 agonist[1][2].
AH-7614 (compound 39) (0.063-1 μM) blocks intracellular Ca2+ response induced by both linoleic acid and FFAR4 agonist in FFA4 expressing U2OS cells[1].
AH-7614 (100 μM) abolishes the enhancement in glucose-stimulated insulin secretion by GSK137647A in NCI-H716 cells[1].
AH-7614 (0.001-10 μM; 15 min) blocks TUG-891-mediated internalization of FFA4 from the cell surface (pIC50=7.70)[2].
AH-7614 (10 μM; 30 min) blocks agonist-induced elevation of intracellular inositol monophosphates and phosphorylation of FFA4[2].
AH7614 (50 μg; intratumoral injection once every 4 d for 20 d) reduces the tumor growth in mice[3].
AH7614 (50 μg; intratumoral injection one day prior to epirubicin injection) enhances cancer cell sensitivity to the chemotherapy and inhibits tumor progression by blocking GPR120 signaling in combination with Epirubicin[3].
| Catalog Number | R027960 |
| CAS Number | 6326-06-3 |
| Synonyms | 4-methyl-N-(9H-xanthen-9-yl)benzenesulfonamide |
| Molecular Formula | C20H17NO3S |
| Purity | ≥95% |
| InChI | InChI=1S/C20H17NO3S/c1-14-10-12-15(13-11-14)25(22,23)21-20-16-6-2-4-8-18(16)24-19-9-5-3-7-17(19)20/h2-13,20-21H,1H3 |
| InChIKey | OZCQEUZTOAAWDK-UHFFFAOYSA-N |
| SMILES | CC1=CC=C(C=C1)S(=O)(=O)NC2C3=CC=CC=C3OC4=CC=CC=C24 |
| Reference | [1]. Sparks SM, et, al. Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120). Bioorg Med Chem Lett. 2014 Jul 15;24(14):3100-3. [2]. Watterson KR, et, al. Probe-Dependent Negative Allosteric Modulators of the Long-Chain Free Fatty Acid Receptor FFA4. Mol Pharmacol. 2017 Jun;91(6):630-641. [3]. Wang X, et, al. Fatty acid receptor GPR120 promotes breast cancer chemoresistance by upregulating ABC transporters expression and fatty acid synthesis. EBioMedicine. 2019 Feb;40:251-262. |
