GLPG-0974 | B3292

GLPG-0974 is a potent FFA2 (free fatty acid receptor 2) antagonist (IC50 = 9 nM). Displays selectivity for FFA2 over FFA3. GLPG-0974 inhibits acetate-induced migration of isolated human neutrophils in buffer or plasma (IC50s = 27 and 43 nM, respectively), as well as acetate-induced expression of CD11b activation-specific epitope on neutrophils in isolated human whole blood (IC50 = 438 nM).

GLPG-0974 is a potent FFA2 (free fatty acid receptor 2) antagonist (IC50 = 9 nM). Displays selectivity for FFA2 over FFA3. GLPG-0974 inhibits acetate-induced migration of isolated human neutrophils in buffer or plasma (IC50s = 27 and 43 nM, respectively), as well as acetate-induced expression of CD11b activation-specific epitope on neutrophils in isolated human whole blood (IC50 = 438 nM).

B3292 | GLPG-0974 DataSheet

Alternate Name/Synonyms: 4-[[[(2R)-1-(Benzo[b]thien-3-ylcarbonyl)-2-methyl-2-azetidinyl]carbonyl][(3-chlorophenyl)methyl]amino]butanoic acid GLPG0974

Appearance: White solid

Formulation:

CAS Number: 1391076-61-1

Structure Available?: Yes

Peptide sequence: N/A

Salt Form: No

Molecular Formula: C₂₅H₂₅ClN₂O₄S

Molecular Weight: 485

Cell-Permeable?: True

Purity: ≥98% by HPLC

Solubilities: >40 mg/ml DMSO >40 mg/ml Ethanol

Handling: Do not take internally. Wear gloves and mask when handling the product! Avoid contact by all modes of exposure.

Country of Origin: USA

Tag Line: A free fatty acid receptor-2 (FFA2/GPR43) antagonist

MDL Number:

PubChem CID: 57520598

SMILES: O=C(N1CC[C@]1(C)C(N(CC2=CC(Cl)=CC=C2)CCCC(O)=O)=O)C3=CSC4=C3C=CC=C4

InChi: InChI=1S/C25H25ClN2O4S/c1-25(11-13-28(25)23(31)20-16-33-21-9-3-2-8-19(20)21)24(32)27(12-5-10-22(29)30)15-17-6-4-7-18(26)14-17/h2-4,6-9,14,16H,5,10-13,15H2,1H3,(H,29,30)/t25-/m1/s1

InChi Key: MPMKMQHJHDHPBE-RUZDIDTESA-N