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Biological Activity for PF 04418948
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).
Sold for research purposes under agreement from Pfizer Inc.
External Portal Information for PF 04418948
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.
Compound Libraries for PF 04418948
Technical Data for PF 04418948
|Storage||Store at -20°C|
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.
Solubility Data for PF 04418948
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for PF 04418948
The following data is based on the product molecular weight 409.41. Batch specific molecular weights may vary from batch to batch due to the degree 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 for PF 04418948
References are publications that support the biological activity of the product.
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
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Keywords: PF 04418948, PF 04418948 supplier, PF04418948, prostanoid, receptors, EP2, antagonists, potent, selective, PGE2, prostaglandins, PTGER2, Prostanoid, Receptors, 4818, Tocris Bioscience
5 Citations for PF 04418948
Citations are publications that use Tocris products. Selected citations for PF 04418948 include:
Guillem-Llobat et al (2016) Aspirin prevents colorectal cancer metastasis in mice by splitting the crosstalk between platelets and tumor cells. Oncotarget 7 32462 PMID: 27074574
Liu et al (2016) Oxidized phospholipid OxPAPC activates TRPA1 and contributes to chronic inflammatory pain in mice PLoS One 11 e0165200 PMID: 27812120
Perkins et al (2018) Autocrine-paracrine prostaglandin E2 signaling restricts TLR4 internalization and TRIF signaling. Nat.Immunol. 19 1309 PMID: 30397349
Liu et al (2016) Inhibition of lysyl oxidase by prostaglandin E2 via EP2/EP4 receptors in human amnion fibroblasts: Implications for parturition. Mol Cell Endocrinol 424 118 PMID: 26826430
Wang et al (2015) Phosphorylation of STAT3 mediates the induction of cyclooxygenase-2 by cortisol in the human amnion at parturition. Sci Signal 8 PMID: 26508788
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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.