PF 04418948 structure
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Common Name | PF 04418948 | ||
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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 04418948PF-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] |
Name | 1-(4-fluorobenzoyl)-3-[(6-methoxynaphthalen-2-yl)oxymethyl]azetidine-3-carboxylic acid |
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Synonym | More Synonyms |
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] |
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Related Catalog | |
References |
Density | 1.4±0.1 g/cm3 |
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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℃ |
RIDADR | NONH for all modes of transport |
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~83% 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 1 | |
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DownStream 0 |
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 |