GLPG 0974

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Cat.No. 5621 - GLPG 0974 | C25H25ClN2O4S | CAS No. 1391076-61-1
Description: Potent FFA2 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)
Datasheet
Citations
Literature

Biological Activity

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.

Technical Data

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
1eq. NaOH 9.7 20mM with gentle warming
DMSO 48.5 100
ethanol 48.5 100

Preparing Stock Solutions

The following data is based on the product molecular weight 485. Batch specific molecular weights may vary from batch to batch due to solvent 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

Safety Datasheet

References

References are publications that support the products' biological activity.

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


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