Home Metabolism FAAH inhibitor PF-04457845

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PF-04457845 FAAH inhibitor

Cat.No.S2421

PF-04457845 (PF-4457845) is a potent, favorable selective inhibitor of Fatty acid amide hydrolase (FAAH) with IC50 of 7.2 nM and 7.4 nM for hFAAH and rFAAH, respectively. This compound covalently modifies the active-site serine nucleophile of FAAH with exquisite selectivity relative to other members of the serine hydrolase superfamily.
PF-04457845 FAAH inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 455.43

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: S242101 DMSO]91 mg/mL]false]Ethanol]4 mg/mL]false]Water]Insoluble]false Purity: 99.65%
99.65

Chemical Information, Storage & Stability

Molecular Weight 455.43 Formula

C23H20F3N5O2

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 1020315-31-4 -- Storage of Stock Solutions

Synonyms PF-4457845 Smiles C1CN(CCC1=CC2=CC(=CC=C2)OC3=NC=C(C=C3)C(F)(F)F)C(=O)NC4=NN=CC=C4

Solubility

In vitro
Batch:

DMSO : 91 mg/mL (199.81 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 4 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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%DMSO %

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Working concentration: mg/ml;

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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC50/Ki
FAAH (human) [1]
(Cell-free assay)
7.2 nM
FAAH (rat) [1]
(Cell-free assay)
7.4 nM
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01092845 Completed
Healthy|Sleep
Pfizer
 April 2010 Phase 1
NCT01002625 Terminated
Sleep|Healthy Volunteers
Pfizer
 November 2009 Phase 1
NCT00981357 Completed
Osteoarthritis Knee
Pfizer
 November 2009 Phase 2
NCT00836082 Completed
Acute Pain|Chronic Pain
Pfizer
 February 2009 Phase 1

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