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PF-3845 FAAH inhibitor

Cat.No.S2666

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

Chemical Structure

Molecular Weight: 456.46

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Quality Control

Batch: Purity: 99.97%
99.97

Solubility

In vitro
Batch:

DMSO : 91 mg/mL (199.36 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous 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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Chemical Information, Storage & Stability

Molecular Weight 456.46 Formula

C24H23F3N4O2

Storage (From the date of receipt)
CAS No. 1196109-52-0 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles C1CN(CCC1CC2=CC(=CC=C2)OC3=NC=C(C=C3)C(F)(F)F)C(=O)NC4=CN=CC=C4

Mechanism of Action

Targets/IC50/Ki
FAAH
230 nM(Ki)
In vitro

PF-3845 selectively inhibits FAAH by carbamylating FAAH's serine nucleophile.

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. This compound shows a long duration of action up to 24 hour. This compound-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. This chemical (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 this chemical). At higher doses (10 and 30 mg/kg), this compound inhibits pain responses to an equivalent, if not greater, degree than the nonsteroidal anti-inflammatory drug naproxen (10mg/kg, p.o.). This chemical (10 mg/kg, i.p.) significantly reverses LPS-induced tactile allodynia, but doesn't modify paw withdrawal thresholds in the saline-injected paw.

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