GLPG 0974

Name: GLPG 0974
Brand: Tocris Bioscience
SKU: 5621

Tocris Bioscience, part of Bio-Techne | Catalog # 5621

Citations (27)

COA / SDS

Potent FFA2 (GPR43) antagonist

Key Product Details

Description:	Potent FFA2 (GPR43) antagonist
Chemical Name:	4-[[[(2R)-1-(Benzo[b]thien-3-ylcarbonyl)-2-methyl-2-azetidinyl]carbonyl][(3-chlorophenyl)methyl]amino]butanoic acid
Purity:	≥98% (HPLC)
Molecular Weight:	485

View Full Technical Details for GLPG 0974

Technical Data
Citations

Biological Activity for GLPG 0974

GLPG 0974 is a potent FFA2 antagonist (IC₅₀ = 9 nM). Exhibits selectivity for FFA2 over FFA3. Inhibits acetate-induced human neutrophil migration in plasma or buffer. Also inhibits FFA2-induced expression of CD11b activation-specific epitope (AE) in human whole blood. Orally bioavailable.

Compound Libraries for GLPG 0974

GLPG 0974 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for GLPG 0974

M. Wt	485
Formula	C₂₅H₂₅ClN₂O₄S
Storage	Store at +4°C
Purity	≥98% (HPLC)
CAS Number	1391076-61-1
PubChem ID	57520598
InChi Key	MPMKMQHJHDHPBE-RUZDIDTESA-N
Smiles	O=C(N1[C@](C(N(CC2=CC(Cl)=CC=C2)CCCC(O)=O)=O)(C)CC1)C3=CSC4=C3C=CC=C4

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for GLPG 0974

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	48.5	100
	ethanol	48.5	100

Preparing Stock Solutions for GLPG 0974

The following data is based on the product molecular weight 485.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.06 mL	10.31 mL	20.62 mL
5 mM	0.41 mL	2.06 mL	4.12 mL
10 mM	0.21 mL	1.03 mL	2.06 mL
50 mM	0.04 mL	0.21 mL	0.41 mL

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References for GLPG 0974

References are publications that support the biological activity of the product.

Pizzonero Discovery and optimization of an azetidine chemical series as a free fatty acid receptor 2 (FFA2) antagonist: from hit to clinic. J.Med.Chem. 2014 PMID: 25380412