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Submit ReviewGLPG 0974
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)
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.
Compound Libraries
GLPG 0974 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| 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 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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Product Datasheets
References
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
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Keywords: GLPG 0974, GLPG 0974 supplier, GLPG0974, free, fatty, acid, receptors, FFA2, antagonists, antagonism, potent, Free, Fatty, Acid, Receptors, 5621, Tocris Bioscience
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