Home Metabolism FAAH inhibitor PF-3845 For research use only.

PF-3845

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

PF-3845 Chemical Structure

PF-3845 Chemical Structure

CAS No. 1196109-52-0

Purity & Quality Control

PF-3845 Related Products

Signaling Pathway

FAAH Signaling Pathways

FAAH Signaling Pathway

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
In vitro

PF-3845 selectively inhibits FAAH by carbamylating FAAH's serine nucleophile. [1]
In Vivo
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 ( [PEA] and [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]
Animal Research Animal Models Male C57BL/6 mice
Dosages 10 mg/kg or 1-30 mg/kg
Administration Administered via i.p. 1 hour before sacrificed by CO2 or oral administration.

Chemical Information & Solubility

Molecular Weight 456.46 Formula

C24H23F3N4O2

CAS No. 1196109-52-0 SDF Download PF-3845 SDF
Smiles C1CN(CCC1CC2=CC(=CC=C2)OC3=NC=C(C=C3)C(F)(F)F)C(=O)NC4=CN=CC=C4
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 91 mg/mL ( (199.36 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 91 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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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

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