PF-4693627 is a potent, selective and orally bioavailable microsomal prostaglandin E synthase-1 (mPGES-1) inhibitor (IC 50 =3 nM) for the treatment of inflammation caused by osteoarthritis (OA) and rheumatoid arthritis (RA).
性状
Solid
IC50 & Target[1][2]
IC50: 3 nM (mPGES-1)
体外研究(In Vitro)
PF-4693627 also inhibits mPGES-1 with IC50s of 180 and 6 nM in HWB-1483 and human fetal fibroblast, respectively.PF-4693627 shows high activity in lipopolysaccharide (LPS) stimulated human whole blood (HWB) cell assay (IC50=109 nM). has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(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.
PF-4693627 (1.0 mg/kg; i.v.) shows good bioavailability (59%) and modest half life (t 1/2 =3.7 h) in Sprague-Dawley rats. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[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.
溶解度数据
In Vitro: DMSO : 100 mg/mL (199.03 mM; Need ultrasonic)配制储备液