A antagonist of FFAR2/GPR43 (IC50 = 9 nM); selective for FFAR2 over FFAR3 at 50s = 27 and 43 nM

GLPG0974 – 5 mg

Brand:
Cayman
CAS:
1391076-61-1
Storage:
-20
UN-No:
Non-Hazardous - /

GLPG0974 is an antagonist of free fatty acid receptor 2 (FFAR2/GPR43; IC50 = 9 nM).{46506} It is selective for FFAR2 over FFAR3 at concentrations up to 30 μM and over a panel of 55 receptors, ion channels, and transporters at 10 μM. GLPG0974 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). GLPG0974 also inhibits a human FFAR2-based designer receptor exclusively activated by designer drugs (hFFAR2-DREADD; IC50 = 36.31 nM in a cell-based β-arrestin-2 recruitment assay).{46507} It inhibits glucagon-like peptide 1 (GLP-1) secretion induced by the hFFA2-DREADD ligand sorbic acid in isolated colonic crypts from mice expressing hemagglutinin-tagged hFFAR2-DREADD when used at a concentration of 10 μM.  

 

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SKU: 28108 - 5 mg Category:

Description

A antagonist of FFAR2/GPR43 (IC50 = 9 nM); selective for FFAR2 over FFAR3 at 50s = 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); inhibits hFFAR2-DREADD (IC50 = 36.31 nM in a cell-based β-arrestin-2 recruitment assay) inhibits GLP-1 secretion induced by sorbic acid in isolated colonic crypts from mice expressing hFFAR2-DREADD-HA at 10 μM

Formal name: 4-[[[(2R)-1-(benzo[b]thien-3-ylcarbonyl)-2-methyl-2-azetidinyl]carbonyl][(3-chlorophenyl)methyl]amino]-butanoic acid

Synonyms: 

Molecular weight: 485

CAS: 1391076-61-1

Purity: ≥98%

Formulation: A solid

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