PF-3845 Licensed by Pfizer

PF-3845 is a potent, selective and irreversible FAAH inhibitor with Ki of 230 nM.

Catalog No.S2666
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PF-3845 Chemical Structure
Molecular Weight: 456.46

Validation & Quality Control

Quality Control & MSDS

Related Compound Libraries

Product Information

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  • PF-3845 Mechanism

Product Description

Biological Activity

Description PF-3845 is a potent, selective and irreversible FAAH inhibitor with Ki of 230 nM.
Targets FAAH
IC50 230 nM (Ki) [1]
In vitro PF-3845 selectively inhibits FAAH by carbamylating FAAH's serine nucleophile. [1]
In vivo PF-3845 treated mice (10 mg/kg, i.p.) shows rapid and complete inactivation of FAAH in the brain, as judged by competitive activity-based protein profiling (ABPP) with the serine hydrolase-directed probe fluorophosphonate (FP)-rhodamine. PF-3845 shows a long duration of action up to 24 hour. PF-3845-treated mice also shows dramatic (>10-fold) elevation in brain levels of AEA and other NAEs (N-pamitoyl ethanolamine [PEA] and N-oleoyl ethanolamine [OEA]). FAAH is AEA-degrading enzyme fatty acid amide hydrolase. PF-3845 (1–30 mg/kg, oral administration [p.o.]) causes a dose dependent inhibition of mechanical allodynia with a minimum effective dose (MED) of 3 mg/kg (rats are analyzed at 4 hour post dosing with PF-3845). At higher doses (10 and 30 mg/kg), PF-3845 inhibits pain responses to an equivalent, if not greater, degree than the nonsteroidal anti-inflammatory drug naproxen (10mg/kg, p.o.). [1] PF-3845 (10 mg/kg, i.p.) significantly reverses LPS-induced tactile allodynia, but doesn't modify paw withdrawal thresholds in the saline-injected paw. [2]
Clinical Trials
Features

Protocol(Only for Reference)

Kinase Assay: [1]

FAAH Assay The GDH-coupled FAAH assay is performed for determination of potencies (Kinact/ Ki values) of irreversible inhibitors. For the development of structure-activity relationship, the FAAH assay is performed in 384-well microplates with a final volume of 50μL. In the 384-well format assay, the overall potency, Kinact/ Ki values, are generally calculated from the slope, Kinact/[ Ki (1 + [S]/ Km)], which is obtained from the kobs versus [I] linear lines under the conditions of [I] << Ki as described (from the kobs values fitted to equation 3 in PNAS 2008). In order to obtain Kinact and Ki values separately for PF-3845 and URB597, the FAAH assay is performed in the 96-well format with a final volume of 200μL. Due to its more frequent reading capabilities (every 10 and 30 seconds for the 96- and 384-well formats, respectively), the 96- well format allows a measurement of Kobs values at higher concentrations of inhibitors. The Kinact and Ki values are obtained by fitting the kobs versus [I] curves to the equation, Kobs = Kinact [I]/{[I] + Ki (1 + [S]/ Km}. FAAH inactivation rates in the absence of inhibitors are subtracted from all kobs values obtained in the presence of inhibitors. The ratio Kinact/ Ki calculated from the individual Kinact and Ki values obtained separately agrees well with the Kinact/ Ki value obtained from the slope described above.

Animal Study: [1]

Animal Models Male C57BL/6 mice
Formulation PF-3845 is dissolved at 1 mg/ml by sonication and vortexing directly into a solution of 18:1:1 v/v/v saline:emulphor:ethanol.
Dosages 10 mg/kg or 1-30 mg/kg
Administration Administered via i.p. 1 hour before sacrificed by CO2 or oral administration.
1

References

Chemical Information

Download PF-3845 SDF
Molecular Weight (MW) 456.46
Formula

C24H23F3N4O2

CAS No. 1196109-52-0
Synonyms N/A
Solubility (25°C)
  • DMSO 91 mg/mL
  • Water <1 mg/mL
  • Ethanol 91 mg/mL
Storage 2 years -20°CPowder
2 weeks4°Cin DMSO
6 months-80°Cin DMSO
Chemical Name 4-(3-(5-(trifluoromethyl)pyridin-2-yloxy)benzyl)-N-(pyridin-3-yl)piperidine-1-carboxamide

Research Area

Tech Support & FAQs

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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