PF-4693627 is a potent, selective and orally bioavailable microsomal prostaglandin E synthase-1 ( m PGES-1 ) inhibitor ( IC 50 =3 nM) for the treatment of inflammation caused by osteoarthritis (OA) and rheumatoid arthritis (RA).
Storage Temp
Store at -20°C
Shipped In
Ice chest + Ice pads
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Product Description
PF-4693627 is a potent, selective and orally bioavailable microsomal prostaglandin E synthase-1 ( m PGES-1 ) inhibitor ( IC 50 =3 nM) for the treatment of inflammation caused by osteoarthritis (OA) and rheumatoid arthritis (RA)
In Vitro
PF-4693627 also inhibits mPGES-1 with IC 50 s 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 (IC 50 =109 nM). MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Guinea pig with carrageenan stimulated air pouch inflammation model Dosage: 10 mg/kg Administration: Administered orally Result: 63% PGE2 inhibition. Animal Model: Sprague-Dawley rats . Dosage: 1.0 mg/kg (Pharmacokinetic Analysis) Administration: Administered i.v. Result: Clearance (CL), volume of distribution (Vd ss ), t 1/2 , mean residence time (MRT) and bioavailability (F) is 12 mL/min/kg, 3.0 L/kg, 3.7 h, 4.42 h, 59%, respectively.
This compound belongs to the class of organic compounds known as polychlorinated biphenyls. These are organic compounds containing at least two chlorine atoms attached to either benzene ring of the biphenyl moiety.
External Descriptors
Not available
1. Djoumbou Feunang Y, Eisner R, Knox C, Chepelev L, Hastings J, Owen G, Fahy E, Steinbeck C, Subramanian S, Bolton E, Greiner R, and Wishart DS. ClassyFire: Automated Chemical Classification With A Comprehensive, Computable Taxonomy. Journal of Cheminformatics, 2016, 8:61.
