PF-3845

Licensed by Pfizer Catalog No.S2666

PF-3845 Chemical Structure

Molecular Weight(MW): 456.46

PF-3845 is a potent, selective and irreversible FAAH inhibitor with Ki of 230 nM, showing negligible activity against FAAH2.

Size Price Stock Quantity  
In DMSO USD 160 In stock
USD 120 In stock
USD 470 In stock
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Biological Activity

Description PF-3845 is a potent, selective and irreversible FAAH inhibitor with Ki of 230 nM, showing negligible activity against FAAH2.
Targets
FAAH [1]
230 nM(Ki)
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]

Protocol

Animal Research:[1]
+ Expand
  • 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.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 91 mg/mL (199.36 mM)
Ethanol 91 mg/mL (199.36 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
30% propylene glycol, 5% Tween 80, 65% D5W
For best results, use promptly after mixing.
15 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 456.46
Formula

C24H23F3N4O2

CAS No. 1196109-52-0
Storage powder
in solvent
Synonyms N/A

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Tech Support

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.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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FAAH Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID