AH-7614 is a potent and specific FFA4 (GPR120) antagonist (inhibitor) with pIC50s of 7.1, 8.1 and 8.1 for human, mouse and rat FFA4, respectively. AH-7614 is more selective for FFA4 than FFA1 (pIC50<4.6). AH-7614 blocks the effects of the polyunsaturated omega-6 fatty acid linoleic acid and FFA4 agonists.

Physicochemical Properties

Molecular Formula	C20H17NO3S
Molecular Weight	351.42
Exact Mass	351.093
Elemental Analysis	C, 68.36; H, 4.88; N, 3.99; O, 13.66; S, 9.12
CAS #	6326-06-3
PubChem CID	233085
Appearance	White to off-white solid powder
Density	1.37g/cm3
Boiling Point	505.9ºC at 760mmHg
Flash Point	259.8ºC
Index of Refraction	1.685
LogP	5.64
Hydrogen Bond Donor Count	1
Hydrogen Bond Acceptor Count	4
Rotatable Bond Count	3
Heavy Atom Count	25
Complexity	528
Defined Atom Stereocenter Count	0
InChi Key	OZCQEUZTOAAWDK-UHFFFAOYSA-N
InChi Code	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
Chemical Name	4-methyl-N-(9H-xanthen-9-yl)benzenesulfonamide
Synonyms	AH-7614 AH7614 AH 7614
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

ln Vitro	In U2OS cells expressing FFA4, AH-7614 (Compound 39) (0.063-1 μM) inhibits the intracellular Ca2+ response brought on by linoleic acid and FFAR4 agonist [1]. In NCI-H716 cells, the increasing impact of GSK137647A on glucose-stimulated insulin production was eliminated by AH-7614 (100 μM) [1]. TUG-891-mediated internalization of FFA4 from the cell surface is blocked by AH-7614 (0.001-10 μM; 15 minutes) (pIC50=7.70) [2]. AH-7614 (10 μM; 30 minutes) inhibits intracellular myo-inositol monophosphate and FFA4 phosphorylation increases brought on by agonists [2].
ln Vivo	In mice, AH7614 (50 μg administered intraperitoneally every 4 μd for 20 days) can inhibit the formation of tumors [3]. ? When paired with epirubicin, AH7614 (50 μg; intratumoral injection given one day prior to the latter) can increase the susceptibility of cancer cells to chemotherapy by blocking GPR120 signaling and preventing tumor growth [3].
References	[1]. 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]. Probe-Dependent Negative Allosteric Modulators of the Long-Chain Free Fatty Acid Receptor FFA4. Mol Pharmacol. 2017 Jun;91(6):630-641. [3]. Fatty acid receptor GPR120 promotes breast cancer chemoresistance by upregulating ABC transporters expression and fatty acid synthesis. EBioMedicine. 2019 Feb;40:251-262.

Solubility Data

Solubility (In Vitro)

DMSO : ~100 mg/mL (~284.56 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.5 mg/mL (7.11 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.8456 mL	14.2280 mL	28.4560 mL
	5 mM	0.5691 mL	2.8456 mL	5.6912 mL
	10 mM	0.2846 mL	1.4228 mL	2.8456 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.