PF 04418948

Modify Date: 2024-01-04 19:46:20

PF 04418948 Structure
PF 04418948 structure
Common Name PF 04418948
CAS Number 1078166-57-0 Molecular Weight 409.407
Density 1.4±0.1 g/cm3 Boiling Point 639.1±55.0 °C at 760 mmHg
Molecular Formula C23H20FNO5 Melting Point N/A
MSDS Chinese USA Flash Point 340.3±31.5 °C

 Use of PF 04418948


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 nMTarget: EP2in 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]

 Names

Name 1-(4-fluorobenzoyl)-3-[(6-methoxynaphthalen-2-yl)oxymethyl]azetidine-3-carboxylic acid
Synonym More Synonyms

 PF 04418948 Biological Activity

Description 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 nMTarget: EP2in 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]
Related Catalog
References

[1]. af Forselles KJ, et al. In vitro and in vivo characterization of PF-04418948, a novel, potent and selective prostaglandin EP2 receptor antagonist. Br J Pharmacol. 2011 Dec;164(7):1847-1856.

[2]. Birrell MA, et al. Selectivity profiling of the novel EP2 receptor antagonist, PF-04418948, in functional bioassay systems: atypical affinity at the guinea pig EP2 receptor. Br J Pharmacol. 2013 Jan;168(1):129-138.

 Chemical & Physical Properties

Density 1.4±0.1 g/cm3
Boiling Point 639.1±55.0 °C at 760 mmHg
Molecular Formula C23H20FNO5
Molecular Weight 409.407
Flash Point 340.3±31.5 °C
Exact Mass 409.132538
PSA 76.07000
LogP 3.08
Vapour Pressure 0.0±2.0 mmHg at 25°C
Index of Refraction 1.639
Storage condition -20℃

 Safety Information

RIDADR NONH for all modes of transport

 Synthetic Route

~83%

PF 04418948 Structure

PF 04418948

CAS#:1078166-57-0

Literature: Pfizer Inc Patent: US2008/280877 A1, 2008 ; Location in patent: Page/Page column 22 ; US 20080280877 A1

 Precursor & DownStream

Precursor  1

DownStream  0

 Synonyms

1-(4-Fluorobenzoyl)-3-{[(6-methoxy-2-naphthyl)oxy]methyl}-3-azetidinecarboxylic acid
pf-04418948
3-Azetidinecarboxylic acid, 1-(4-fluorobenzoyl)-3-[[(6-methoxy-2-naphthalenyl)oxy]methyl]-
unii-i7z38e70vf
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