1078166-57-0 Usage
Uses
Used in Pharmaceutical Industry:
PF 04418948 is used as a pharmaceutical agent for its potent and selective antagonistic action on the prostaglandin EP2 receptor. This property makes it a valuable compound in the development of treatments for various conditions, as modulation of the prostaglandin EP2 receptor can have therapeutic effects.
Used in Research Applications:
PF 04418948 is used as a research tool in TG (trigeminal ganglion) explant culture. Its selective antagonism of the prostaglandin EP2 receptor allows researchers to study the role of this receptor in various biological processes and conditions, contributing to a better understanding of its potential applications in medicine.
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 ep? 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. s?fholm 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.
Check Digit Verification of cas no
The CAS Registry Mumber 1078166-57-0 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,0,7,8,1,6 and 6 respectively; the second part has 2 digits, 5 and 7 respectively.
Calculate Digit Verification of CAS Registry Number 1078166-57:
(9*1)+(8*0)+(7*7)+(6*8)+(5*1)+(4*6)+(3*6)+(2*5)+(1*7)=170
170 % 10 = 0
So 1078166-57-0 is a valid CAS Registry Number.
