GLPG 0974

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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)
Citations (2)

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
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 Data for GLPG 0974

Solvent Max Conc. mg/mL Max Conc. mM
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.

Select a batch to recalculate based on the batch molecular weight:
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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Product Datasheets for GLPG 0974

Certificate of Analysis / Product Datasheet
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References for GLPG 0974

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

Pizzonero et al (2014) Discovery and optimization of an azetidine chemical series as a free fatty acid receptor 2 (FFA2) antagonist: from hit to clinic. J.Med.Chem. 57 10044 PMID: 25380412

If you know of a relevant reference for GLPG 0974, please let us know.

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2 Citations for GLPG 0974

Citations are publications that use Tocris products. Selected citations for GLPG 0974 include:

Marco et al (2020) Acetate coordinates neutrophil and ILC3 responses against C. difficile through FFAR2. J Exp Med 217 PMID: 31876919

Tsung-Hsien et al (2020) Leuconostoc mesenteroides fermentation produces butyric acid and mediates Ffar2 to regulate blood glucose and insulin in type 1 diabetic mice. Sci Rep 10 7928 PMID: 32404878

Do you know of a great paper that uses GLPG 0974 from Tocris? Please let us know.

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