Chemical Name: 1-(4-Fluorobenzoyl)-3-[[(6-methoxy-2-naphthalenyl)oxy]methyl]-3-azetidinecarboxylic acid
Biological ActivityPF 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 InformationThe 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.
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.
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.
In vitro and in vivo characterization of PF-04418948, a novel, potent and selective prostaglandin EP2 receptor antagonist.
af Forselles et al.
Citations for PF 04418948
The citations listed below are publications that use Tocris products. Selected citations for PF 04418948 include:
5 Citations: Showing 1 - 5
Autocrine-paracrine prostaglandin E2 signaling restricts TLR4 internalization and TRIF signaling.
Authors: Perkins Et al.
Aspirin prevents colorectal cancer metastasis in mice by splitting the crosstalk between platelets and tumor cells.
Authors: Guillem-Llobat Et al.
Inhibition of lysyl oxidase by prostaglandin E2 via EP2/EP4 receptors in human amnion fibroblasts: Implications for parturition.
Authors: Liu Et al.
Mol Cell Endocrinol 2016;424:118
Oxidized phospholipid OxPAPC activates TRPA1 and contributes to chronic inflammatory pain in mice
Authors: Liu Et al.
PLoS One 2016;11:e0165200
Phosphorylation of STAT3 mediates the induction of cyclooxygenase-2 by cortisol in the human amnion at parturition.
Authors: Wang Et al.
Sci Signal 2015;8
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in vivo survival assay