Home Metabolism FAAH inhibitor PF-04457845 For research use only.

PF-04457845

Synonyms: PF-4457845

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. PF-04457845 covalently modifies the active-site serine nucleophile of FAAH with exquisite selectivity relative to other members of the serine hydrolase superfamily.

PF-04457845 Chemical Structure

PF-04457845 Chemical Structure

CAS No. 1020315-31-4

Purity & Quality Control

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

PF-04457845 Related Products

Signaling Pathway

FAAH Signaling Pathways

FAAH Signaling Pathway

Biological Activity

Description 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. PF-04457845 covalently modifies the active-site serine nucleophile of FAAH with exquisite selectivity relative to other members of the serine hydrolase superfamily.
Targets
FAAH (human) [1]
(Cell-free assay)		 FAAH (rat) [1]
(Cell-free assay)
7.2 nM 7.4 nM
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

Chemical Information & Solubility

Molecular Weight 455.43 Formula

C23H20F3N5O2
CAS No. 1020315-31-4 SDF --
Smiles C1CN(CCC1=CC2=CC(=CC=C2)OC3=NC=C(C=C3)C(F)(F)F)C(=O)NC4=NN=CC=C4
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 91 mg/mL ( (199.81 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 4 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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