For research use only. Not for therapeutic Use.
PF-4693627 is a potent, selective and orally bioavailable microsomal prostaglandin E synthase-1 (mPGES-1) inhibitor (IC50=3 nM) for the treatment of inflammation caused by osteoarthritis (OA) and rheumatoid arthritis (RA)[1].
PF-4693627 also inhibits mPGES-1 with IC50s of 180 and 6 nM in HWB-1483 and human fetal fibroblast, respectively[1].
PF-4693627 shows high activity in lipopolysaccharide (LPS) stimulated human whole blood (HWB) cell assay (IC50=109 nM)[1].
PF-4693627 (10 mg/kg; orally) inhibits 63% of PGE2 production relative to vehicle control in Guinea pig carrageenan stimulated air pouch model[1].
PF-4693627 (1.0 mg/kg; i.v.) shows good bioavailability (59%) and modest half life (t1/2=3.7 h) in Sprague-Dawley rats[1].
| Catalog Number | I011988 |
| CAS Number | 1312815-93-2 |
| Synonyms | 1-[5-chloro-6-(4-chlorophenyl)-1,3-benzoxazol-2-yl]-N-[(1S,3S)-3-(hydroxymethyl)cyclohexyl]piperidine-4-carboxamide |
| Molecular Formula | C26H29Cl2N3O3 |
| Purity | ≥95% |
| InChI | InChI=1S/C26H29Cl2N3O3/c27-19-6-4-17(5-7-19)21-13-24-23(14-22(21)28)30-26(34-24)31-10-8-18(9-11-31)25(33)29-20-3-1-2-16(12-20)15-32/h4-7,13-14,16,18,20,32H,1-3,8-12,15H2,(H,29,33)/t16-,20-/m0/s1 |
| InChIKey | CPDNPVKDQXLYHO-JXFKEZNVSA-N |
| SMILES | C1CC(CC(C1)NC(=O)C2CCN(CC2)C3=NC4=C(O3)C=C(C(=C4)Cl)C5=CC=C(C=C5)Cl)CO |
| Reference | [1]. Arhancet GB, et al. Discovery and SAR of PF-4693627, a potent, selective and orally bioavailable mPGES-1 inhibitor for the potential treatment of inflammation. Bioorg Med Chem Lett. 2013 Feb 15;23(4):1114-9. |
