Specification
Description
AH-7614 is a selective free fatty acid receptor 4 (FFA4/GPR120) antagonist.
Synonyms
AH-7614; AH 7614; AH7614
IUPAC Name
4-Methyl-N-9H-xanthen-9-yl-benzenesulfonamide
Canonical SMILES
O=S(C1=CC=C(C)C=C1)(NC2C3=C(OC4=C2C=CC=C4)C=CC=C3)=O
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
InChI Key
OZCQEUZTOAAWDK-UHFFFAOYSA-N
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Storage
Dry, dark and at 0-4 °C for short term (days to weeks) or -20 °C for long term (months to years).
Biological Target
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, as well as has selectivity for FFA4 over FFA1 (pIC50<4.6).
Drug Formulation
This drug may be formulated in DMSO
Elemental Analysis
C, 68.36; H, 4.88; N, 3.99; O, 13.66; S, 9.12
HS Tariff Code
2934.99.9001
In Vitro Activity
To elucidate the mechanism underlying the inhibitory effect of DHA on cerulein-induced zymogen activation via the GPR120 and GPR40 signaling pathway, we investigated whether a GPR120 antagonist AH-7614 and a GPR40 antagonist DC260126 could suppress this inhibitory effect of DHA. As shown in Fig. Fig.4,4, cerulein stimulation increased zymogen activation, and this was inhibited by DHA. However, AH-7614 suppressed the inhibitory effect of DHA on cerulein-induced zymogen activation.
Reference: Genes Nutr. 2020 Mar 23;15(1):6. https://pubmed.ncbi.nlm.nih.gov/32293245/
In Vivo Activity
To further confirm the requirement of GPR120 and PPARγ in the regulation of IL-1β and NGF production, the antagonists of GPR120 and PPARγ were used in infarcted rats. AH-7614 reversed the attenuated levels of IL-1β levels and NGF compared with EPA or DHA alone, implying that GPR120 is a downstream molecule of ω-3 PUFAs. The relation between both signaling pathways of GPR120 and PPARγ was also assessed. A significant decrease in PPARγ was observed in infarcted hearts infused with a GPR120 antagonist, AH-7614.
Reference: J Nutr Biochem. 2022 Feb 1;103:108950. https://pubmed.ncbi.nlm.nih.gov/35121022/
Shipping
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Stock Solution Storage
0-4 °C for short term (days to weeks), or -20 °C for long term (months).