GLPG 0974
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 | |||
| DMSO | 48.5 | 100 | |
| 1eq. NaOH | 9.7 | 20 with gentle warming |
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.
| 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
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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