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Chemical Structure| 1078166-57-0 Chemical Structure| 1078166-57-0

Structure of PF-04418948
CAS No.: 1078166-57-0

Chemical Structure| 1078166-57-0

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PF-04418948 is an antagonist of prostaglandin EP2 receptor with IC50 of 16 nM.

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Product Details of PF-04418948

CAS No. :1078166-57-0
Formula : C23H20FNO5
M.W : 409.41
SMILES Code : O=C(C1(COC2=CC=C3C=C(OC)C=CC3=C2)CN(C(C4=CC=C(F)C=C4)=O)C1)O
MDL No. :MFCD24387541
InChI Key :LWJGMYMNSNVCEM-UHFFFAOYSA-N
Pubchem ID :25114442

Safety of PF-04418948

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of PF-04418948

GPCR

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Mouse trachea 1.3 nM 30 min To evaluate the antagonistic effect of PF-04418948 on EP2 receptors in mouse trachea, showing effective antagonism of PGE2-induced relaxation. PMC3246710
Dog bronchiole 2.5 nM 1 h To evaluate the antagonistic effect of PF-04418948 on EP2 receptors in dog bronchiole, showing effective antagonism of PGE2-induced relaxation. PMC3246710
Human myometrium 5.4 nM 60 min To evaluate the antagonistic effect of PF-04418948 on EP2 receptors in human myometrium, showing effective antagonism of butaprost-induced contraction inhibition. PMC3246710
CHO cells expressing human EP2 receptor 1.8 nM To evaluate the functional antagonist potency of PF-04418948 on human EP2 receptors, showing potent antagonism. PMC3246710
Human peripheral blood neutrophils 10 nM 3 h To investigate the effect of EP2 receptor antagonist on NETosis, results showed that EP2 antagonist enhanced NETosis in human peripheral blood neutrophils. PMC4731709
Murine neutrophils 10 nM 5 h To investigate the effect of EP2 receptor antagonist on NETosis, results showed that EP2 antagonist enhanced NETosis in murine BMT neutrophils. PMC4731709

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Rats Rat cutaneous blood flow model Oral 10 mg/kg Single dose To evaluate the effect of PF-04418948 on rat cutaneous blood flow, showing significant attenuation of butaprost-induced blood flow response. PMC3246710
Wistar rats Healthy rat retina model Intravitreal injection 20 nmol/eye Single administration To investigate the effect of PF-04418948 on NOR3-induced dilation of retinal arterioles in rats. The results showed that PF-04418948 significantly suppressed the NOR3-induced dilation of retinal arterioles. PMC9599243

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.44mL

0.49mL

0.24mL

12.21mL

2.44mL

1.22mL

24.43mL

4.89mL

2.44mL

References

[1]af Forselles KJ, Root J, 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):1847-56.

[2]Kay LJ, Gilbert M, et al. Characterization of the EP receptor subtype that mediates the inhibitory effects of prostaglandin E2 on IgE-dependent secretion from human lung mast cells. Clin Exp Allergy. 2013 Jul;43(7):741-51.

[3]Birrell MA, Maher SA, 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):129-38.

[4]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. PMID: 22747912; PMCID: PMC3570009.

[5]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. PMID: 21595651; PMCID: PMC3246710.

[6]Kay LJ, Gilbert M, Pullen N, Skerratt S, Farrington J, Seward EP, Peachell PT. Characterization of the EP receptor subtype that mediates the inhibitory effects of prostaglandin E2 on IgE-dependent secretion from human lung mast cells. Clin Exp Allergy. 2013 Jul;43(7):741-51. doi: 10.1111/cea.12142. PMID: 23786281.

 

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