Catalog Number: 4818
Chemical Name: 1-(4-Fluorobenzoyl)-3-[[(6-methoxy-2-naphthalenyl)oxy]methyl]-3-azetidinecarboxylic acid
Biological Activity
Potent EP2 receptor antagonist (IC50 = 16 nM for human EP2 receptors). Displays over 2000-fold selectivity for EP2 receptors over EP1, EP3, EP4, DP1 amd CRTH2 receptors; exhibits <30% binding at a diverse panel of GPCRs and ion channels at a concentration of 10 μM. Inhibits PGE2-induced increases in intracellular cAMP; reverses PGE2-invoked relaxation of mouse trachea (IC50 = 2.7 nM).
Technical Data
  • M.Wt:
    409.41
  • Formula:
    C23H20FNO5
  • Solubility:
    Soluble to 100 mM in DMSO
  • Purity:
    >99%
  • Storage:
    Store at -20°C
  • CAS No:
    1078166-57-0
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Additional Information
Licensing Caveats:
Sold for research purposes under agreement from Pfizer Inc.
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
Citations:

The citations listed below are publications that use Tocris products. Selected citations for PF 04418948 include:

1 Citations: Showing 1 - 1

  1. Oxidized phospholipid OxPAPC activates TRPA1 and contributes to chronic inflammatory pain in mice
    Authors: Liu Et al.
    PLoS One 2016;11:e0165200
Average Rating: 5 (Based on 1 review)

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Other Experimental Details

Other Experimental Detailsin vivo survival assay

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