PF-04418948_1078166-57-0_DataSheet_MedChemExpress

Product Data SheetProduct Name:CAS No.: Cat. No.:MWt:Formula:Purity :PF-044189481078166-57-0HY-18966409.41C23H20FNO5>98%Solubility:10 mM in DMSOMechanisms: Pathways:GPCR/G protein; Target:Prostaglandin Receptor Biological Activity:PF04418948 is a novel, potent and selective prostaglandin EP2 receptor antagonist with IC50 of 16PF-04418948isanovel,potentandselectiveprostaglandinEP2receptorantagonistwithIC50of16nM, displays >2000-fold functional selectivity for the human EP2 receptor over antagonist activityagainst the human EP1, EP3, EP4, DP1 and CRTH2 receptors. IC50 value: 16 nM Target: EP2 in vitro: PF-04418948 inhibits prostaglandin E2 (PGE2)-induced increase in cAMP in cellsexpressing EP2 receptors with a functional KB value of 1.8 nM. In human myometrium, PF-04418948 produced a parallel, rightward shift of the butaprost-induced inhibition of the contractionsinduced by electrical field stimulation with an apparent KB of 5.4 nM. [1] in vivo: In dog bronchiole and mouse trachea, PF-04418948 produced parallel rightward shifts of thePGE2-induced relaxation curve with a KB of 2.5 nM and an apparent KB of 1.3 nM respectively.Reversal of the PGE2-induced relaxation in the ...References:[1]. af Forselles KJ, et al. In vitro and in vivo characterization of PF-04418948, a novel, potent andselective prostaglandin EP2 receptor antagonist. Br J Pharmacol. 2011 Dec;164(7):1847-1856. [2].BirrellMA,etal.SelectivityprofilingofthenovelEP2receptorantagonist,PF-04418948,[2]. Birrell MA, et al. Selectivity profiling of the novel EP2 receptor antagonist, PF04418948, ininfunctional bioassay systems: atypical affinity at the guinea pig EP2 receptor. Br J Pharmacol. 2013Jan;168(1):129-138. Caution: Not fully tested. For research purposes onlyMedchemexpress LLCwww.medchemexpress.com11DeerParkDrive, Suite 102D Monmouth Junction, NJ 08852,USAail: info@medchemexpress.com Web: www.medchemexpress.comEm