PF 04418948

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Cat.No. 4818 - PF 04418948 | C23H20FNO5 | CAS No. 1078166-57-0
Description: Potent and selective EP2 receptor antagonist
Chemical Name: 1-(4-Fluorobenzoyl)-3-[[(6-methoxy-2-naphthalenyl)oxy]methyl]-3-azetidinecarboxylic acid
Purity: ≥99% (HPLC)
Datasheet
Citations (1)
Literature

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).

Licensing Information

Sold for research purposes under agreement from Pfizer Inc.

Compound Libraries

PF 04418948 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 409.41
Formula C23H20FNO5
Storage Store at -20°C
Purity ≥99% (HPLC)
CAS Number 1078166-57-0
PubChem ID 25114442
InChI Key LWJGMYMNSNVCEM-UHFFFAOYSA-N
Smiles FC(C=C4)=CC=C4C(N(C3)CC3(C(O)=O)COC2=CC1=CC=C(OC)C=C1C=C2)=O

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 40.94 100

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.

Select a batch to recalculate based on the batch molecular weight:
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

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Product Datasheets

Safety Datasheet

References

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


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Keywords: PF04418948 prostanoid receptors EP2 antagonists potent selective PGE2 prostaglandins Prostanoid Receptors

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


Do you know of a great paper that uses PF 04418948 from Tocris? If so please let us know.

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Pathways for PF 04418948

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