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).
Sold for research purposes under agreement from Pfizer Inc.
|Storage||Store at -20°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 409.41. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.44 mL||12.21 mL||24.43 mL|
|5 mM||0.49 mL||2.44 mL||4.89 mL|
|10 mM||0.24 mL||1.22 mL||2.44 mL|
|50 mM||0.05 mL||0.24 mL||0.49 mL|
References are publications that support the products' biological activity.
Birrell et al (2013) 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. 168 129 PMID: 22747912
af Forselles et al (2011) In vitro and in vivo characterization of PF-04418948, a novel, potent and selective prostaglandin EP2 receptor antagonist. Br.J.Pharmacol. 164 1847 PMID: 21595651
If you know of a relevant reference for PF 04418948, please let us know.
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Keywords: PF 04418948, supplier, PF04418948, prostanoid, receptors, EP2, antagonists, potent, selective, PGE2, prostaglandins, Prostanoid, Receptors, Prostanoid, Receptors, Tocris Bioscience
1 Citation for PF 04418948
Citations are publications that use Tocris products. Selected citations for PF 04418948 include:
Liu et al (2016) Oxidized phospholipid OxPAPC activates TRPA1 and contributes to chronic inflammatory pain in mice PLoS One 11 e0165200 PMID: 27812120
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Literature in this Area
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Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.