PF 04418948

Biological Activity

PF 04418948 is a potent prostaglandin E receptor 2 antagonist (PTGER2; EP2; IC₅₀ = 16 nM for human EP₂ receptors), which displays over 2000-fold selectivity for EP₂ receptors over EP₁, EP₃, EP₄, DP₁ amd CRTH₂ receptors and exhibits <30% binding at a diverse panel of GPCRs and ion channels at a concentration of 10 μM. PF 04418948 inhibits PGE₂-induced increases in intracellular cAMP in vitro and reverses PGE₂-invoked relaxation of mouse trachea (IC₅₀ = 2.7 nM).

External Portal Information

The Chemical Probes pages of the Structural Genomics Consortium website are a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of PF 04418948 is reviewed.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Additional Information

Background References

1. Selectivity profiling of the novel EP₂ receptor antagonist, PF-04418948, in functional bioassay systems: atypical affinity at the guinea pig EP₂ receptor.
   Birrell et al.
   Br.J.Pharmacol., 2013;168:129
2. In vitro and in vivo characterization of PF-04418948, a novel, potent and selective prostaglandin EP₂ receptor antagonist.
   af Forselles et al.
   Br.J.Pharmacol., 2011;164:1847

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