receptor antagonist (IC50
= 16 nM for human EP2
receptors). Displays over 2000-fold selectivity for EP2
receptors over EP1
receptors; exhibits <30% binding at a diverse panel of GPCRs and ion channels at a concentration of 10 μ
M. Inhibits PGE2
-induced increases in intracellular cAMP; reverses PGE2
-invoked relaxation of mouse trachea (IC50
= 2.7 nM).
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.
Sold for research purposes under agreement from Pfizer Inc.
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.