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Submit ReviewPF 04457845 is a potent and selective irreversible FAAH inhibitor (IC50 = 7.2 nM, which is selective for FAAH over a panel of other serine hydrolases. PF 04457845 exhibits efficacy in a rat inflammatory pain model, and is orally bioavailable and brain penetrant.
Sold for research purposes under agreement from Pfizer Inc
Chemicalprobes.org and the Chemical Probes webpages of the Structural Genomics Consortium are portals that offer independent guidance on the selection and/or application of small molecules for research. The use of PF 04457845 is reviewed on chemicalprobes.org and the SGC website.
PF 04457845 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
M. Wt | 455.43 |
Formula | C23H20F3N5O2 |
Storage | Store at +4°C |
Purity | ≥98% (HPLC) |
CAS Number | 1020315-31-4 |
PubChem ID | 24771824 |
InChI Key | BATCTBJIJJEPHM-UHFFFAOYSA-N |
Smiles | FC(F)(C1=CC=C(N=C1)OC2=CC=CC(/C=C3CCN(C(NC4=CC=CN=N4)=O)CC\3)=C2)F |
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.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 45.54 | 100 | |
ethanol | 9.11 | 20 |
The following data is based on the product molecular weight 455.43. 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 | 2.2 mL | 10.98 mL | 21.96 mL |
5 mM | 0.44 mL | 2.2 mL | 4.39 mL |
10 mM | 0.22 mL | 1.1 mL | 2.2 mL |
50 mM | 0.04 mL | 0.22 mL | 0.44 mL |
References are publications that support the biological activity of the product.
Ahn et al (2011) Mechanistic and pharmacological characterization of PF-04457845: a highly potent and selective fatty acid amide hydrolase inhibitor that reduces inflammatory and noninflammatory pain. J.Pharmacol.Exp.Ther. 338 114 PMID: 21505060
Johnson et al (2011) Discovery of PF-04457845: a highly potent, orally bioavailable, and selective urea FAAH inhibitor. ACS Med.Chem.Lett. 2 91 PMID: 21666860
If you know of a relevant reference for PF 04457845, please let us know.
Keywords: PF 04457845, PF 04457845 supplier, PF04457845, FAAH, fatty, acid, amide, hydrolase, inhibitors, inhibits, potent, selective, irreversible, orally, bioavailalbe, brain, penetrant, Fatty, Acid, Amide, Hydrolase, (FAAH), 6374, Tocris Bioscience
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The key feature of drug addiction is the inability to stop using a drug despite clear evidence of harm. This poster describes the brain circuits associated with addiction, and provides an overview of the main classes of addictive drugs and the neurotransmitter systems that they target.