GLPG0974

GLPG0974 is an experimental drug which acts as a reasonably potent and selective antagonist for the free fatty acid receptor FFAR2 (GPR43). It was originally developed as a potential medication for ulcerative colitis, and while it was not developed as a medicine for this application it has remained widely used as a pharmacological tool compound for research into the FFAR2 receptor, as one of the relatively few selective FFAR2 antagonists available.^{[1][2][3][4][5]} Despite its antagonist action, it can also act as a positive allosteric modulator of FFAR2 under some conditions, which can complicate interpretation of results obtained using GLPG0974 in the presence of other FFAR2 ligands.^[6]

GLPG0974

Identifiers
IUPAC name 4-[[(2R)-1-(1-benzothiophene-3-carbonyl)-2-methylazetidine-2-carbonyl]-[(3-chlorophenyl)methyl]amino]butanoic acid
CAS Number	1391076-61-1
PubChem CID	57520598
DrugBank	DB15406
ChemSpider	35033253
UNII	X7REK61AIS
ChEMBL	ChEMBL3353541
Chemical and physical data
Formula	C25H25ClN2O4S
Molar mass	485.00 g·mol−1
3D model (JSmol)	Interactive image
SMILES C[C@@]1(CCN1C(=O)C2=CSC3=CC=CC=C32)C(=O)N(CCCC(=O)O)CC4=CC(=CC=C4)Cl
InChI InChI=1S/C21H21ClN2OS/c1-21(2,3)18(15-9-11-16(22)12-10-15)19(25)24-20-23-13-17(26-20)14-7-5-4-6-8-14/h4-13,18H,1-3H3,(H,23,24,25)/t18-/m0/s1 Key:MPMKMQHJHDHPBE-RUZDIDTESA-N