PF 04418948 Property

Melting point:

171-172°C

Boiling point:

639.1±55.0 °C(Predicted)

Density 

1.357±0.06 g/cm3(Predicted)

storage temp. 

room temp

solubility 

DMSO: soluble20mg/mL, clear

form 

powder

pka

3.25±0.20(Predicted)

color 

white to beige

InChIKey

POJZIZBONPAWIV-UHFFFAOYSA-N

Safety

WGK Germany 

3

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

PF 04418948 Chemical Properties,Usage,Production

Chemical Properties

White Solid

Uses

PF-04418948 has been used in TG (trigeminal ganglion) explant culture.

Uses

PF 04418948 acts as a novel, potent and selective prostoglandin EP2 receptor antagonist.

Biological Activity

pf-04418948 is an orally active, potent and selective prostaglandin ep2 receptor antagonist with an ic50 of 16 nm.prostaglandin e2 (pge2) induces distinct responses through four different ‘e prostanoid’ (ep) receptors. ep2 is a g protein-coupled receptor which signals preferentially through gs proteins. it is far less active at other prostanoid receptors, including other ep receptors. pf-04418948 can be used in both cells and tissues.1: af forselles kj, root j, clarke t, davey d, aughton k, dack k, pullen n. 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):1847-56. doi: 10.1111/j.1476-5381.2011.01495.x. erratum in: br j pharmacol. 2012 jun;166(3):1192. dosage error in article text. pubmed pmid: 21595651; pubmed central pmcid: pmc3246710.2. birrell ma, maher sa, buckley j, dale n, bonvini s, raemdonck k, pullen n, giembycz ma, belvisi mg. 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):129-38. doi: 10.1111/j.1476-5381.2012.02088.x. pubmed pmid: 22747912; pubmed central pmcid: pmc3570009.3. säfholm j, dahlén se, delin i, maxey k, stark k, cardell lo, adner m. pge2 maintains the tone of the guinea pig trachea through a balance between activation of contractile ep1 receptors and relaxant ep2 receptors. br j pharmacol. 2013 feb;168(4):794-806. doi: 10.1111/j.1476-5381.2012.02189.x. pubmed pmid: 22934927; pubmed central pmcid: pmc3631371

Biochem/physiol Actions

PF-04418948 is a PGE2 Receptor (EP2) specific antagonist (IC50 = 16 nM) with greater than 2000-fold selectivity over other EP subtypes. PF-04418948 inhibits EP2 activity in smooth muscle preps from human, dog and mouse.

in vitro

pf-04418948 inhibited prostaglandin e2 (pge2)-induced growth in camp with a functional kb value of 1.8 nm in cells expressing ep2 receptors.

in vivo

in the case of human myometrium, pf-04418948 caused a parallel, rightward shift of the butaprost-induced inhibition of the contractions that was induced by electrical field stimulation with an apparent kb of 5.4 nm. in dog bronchiole and mouse trachea, it produced the same shifts of the pge2-induced relaxation curve with a kb of 2.5 nm and an apparent kb of 1.3 nm respectively. moreover, in the mouse trachea, reversal of the pge2-induced relaxation by pf-04418948 produced an ic50 value of 2.7 nm.in rats, pf-04418948 significantly weakens the effects of the ep2-selective agonist butaprost on cutaneous blood flow when given orally. it was selective for ep2 receptors over homologous and unrelated receptors, enzymes and channels.

storage

Store at -20°C