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PF-04418948

Catalog No. T3306   CAS 1078166-57-0
Synonyms: PF 04418948, PF04418948

PF-04418948 is a 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).

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PF-04418948 Chemical Structure
PF-04418948, CAS 1078166-57-0
Pack Size Availability Price/USD Quantity
2 mg In stock $ 40.00
5 mg In stock $ 63.00
10 mg In stock $ 90.00
25 mg In stock $ 196.00
50 mg In stock $ 339.00
100 mg In stock $ 374.00
1 mL * 10 mM (in DMSO) In stock $ 68.00
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Purity: 99.45%
Purity: 99.26%
Purity: 97.61%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description PF-04418948 is a 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).
Targets&IC50 EP2 receptor:16 nM
In vivo Eslicarbazepine acetate(ESL) has Anticonvulsant effects on the development of latrunculin A-induced seizures and paroxysmal EEG activity. ESL may also exhibit disease-modifying effects beyond suppressing just seizure activity, possibly by altering the development of a hyperexcitable network, as evidenced by the suppressed changes in glycine, taurine, glutamate and aspartate concentrations associated with an antiepileptogenic effect[1].
Synonyms PF 04418948, PF04418948
Molecular Weight 409.41
Formula C23H20FNO5
CAS No. 1078166-57-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 40.9 mg/mL (100 mM)

TargetMolReferences and Literature

1. af Forselles KJ, et al. In vitro and in vivo characterization of PF-04418948, a novel, potent and selective prostaglandin EP2 receptor antagonist. Br J Pharmacol. 2011 Dec;164(7):1847-1856 2. Birrell MA, et al. Br J Pharmacol. 2013 Jan;168(1):129-38. 3. Lu W, Yu W, He J, et al. Reprogramming immunosuppressive myeloid cells facilitates immunotherapy for colorectal cancer[J]. EMBO Molecular Medicine. 2020: e12798.

TargetMolCitations

1. Lu W, Yu W, He J, et al. Reprogramming immunosuppressive myeloid cells facilitates immunotherapy for colorectal cancer. EMBO Molecular Medicine. 2020: e12798.

Related compound libraries

This product is contained In the following compound libraries:
Drug Repurposing Compound Library Anti-Cancer Drug Library Inhibitor Library Anti-Cancer Clinical Compound Library GPCR Compound Library Bioactive Compounds Library Max Bioactive Compound Library Anti-Cancer Compound Library Target-Focused Phenotypic Screening Library Orally Active Compound Library

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Keywords

PF-04418948 1078166-57-0 GPCR/G Protein Immunology/Inflammation Prostaglandin Receptor Inhibitor CHO PF 04418948 PF04418948 orally activity inhibit inhibitor

 

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