CAS No. : 1078166-57-0

Product Details
For research use only. Not Intended for Therapeutic Use!
Cat No:I000351
Synonyms:1-(4-fluorobenzoyl)-3-(((6-methoxynaphthalen-2-yl)oxy)methyl)azetidine-3-carboxylic acid
Molecular Formula:C₂₃H₂₀FNO₅
Molecular Weight:409.41
Target:Prostanoid Receptors
IC50:16 nM
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Appearance:Solid powder
Purity: > 98%
Cat No:I000351
Cas No:1078166-57-0

PF-04418948 is a novel, potent and selective prostaglandin EP2 receptor antagonist with IC50 of 16 nM, displays >2000-fold functional selectivity for the human EP2 receptor over antagonist activity against 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 cells expressing 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 contractions induced 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 the PGE2-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 mouse trachea by PF-04418948 produced an IC50 value of 2.7 nM. Given orally, PF-04418948 attenuated the butaprost-induced cutaneous blood flow response in rats. [1] PF-04418948 competitively inhibits relaxations of murine and guinea pig trachea induced by ONO-AE1-259 and PGE2 respectively.[2]

1:Selectivity profiling of the novel EP2 receptor antagonist, PF-04418948, in functional bioassay systems: atypical affinity at the guinea pig EP2 receptor. Birrell MA, Maher SA, Buckley J, Dale N, Bonvini S, Raemdonck K, Pullen N, Giembycz MA, Belvisi MG.Br J Pharmacol. 2013 Jan;168(1):129-38. doi: 10.1111/j.1476-5381.2012.02088.x. PMID: 22747912 Free PMC Article
2:In vitro and in vivo characterization of PF-04418948, a novel, potent and selective prostaglandin EP₂ receptor antagonist. af Forselles KJ, Root J, Clarke T, Davey D, Aughton K, Dack K, Pullen N.Br J Pharmacol. 2011 Dec;164(7):1847-56. doi: 10.1111/j.1476-5381.2011.01495.x. Erratum in: Br J Pharmacol. 2012 Jun;166(3):1192. Dosage error in article text. PMID: 21595651 Free PMC Article
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