| Bioactivity | 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]. | ||||||||||||
| Target | IC50: 3 nM (mPGES-1) | ||||||||||||
| Invitro | 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]. | ||||||||||||
| In Vivo | 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]. Animal Model: | ||||||||||||
| Name | PF-4693627 | ||||||||||||
| CAS | 1312815-93-2 | ||||||||||||
| Formula | C26H29Cl2N3O3 | ||||||||||||
| Molar Mass | 502.43 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
|
||||||||||||
| 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. |
PF-4693627
CAS: 1312815-93-2 F: C26H29Cl2N3O3 W: 502.43
PF-4693627 is a potent, selective and orally bioavailable microsomal prostaglandin E synthase-1 (mPGES-1) inhibitor (IC5
Data collection：peptidedb@qq.com
This product is for research use only, not for human use. We do not sell to patients.