PF-3845A selective and irreversible FAAH inhibitor

PF-3845

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Application: A selective and irreversible FAAH inhibitor
Purity: ≥98%
Molecular Weight: 456.5
Molecular Formula: C24H23F3N4O2
* Refer to Certificate of Analysis for lot specific data (including water content).
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PF-3845 is a piperidine urea compound, which acts as a fatty acid amide hydrolase (FAAH) inhibitor degrading n-acyl ethanolamines (NAEs). Studies suggest that PF-3845 shows an anti-allodynic phenotype in rats. It is known that PF-3845 functions by irreversibly binding to Ser241 of FAAH at the catalytic sites via carbamylation. This causes an increase in arachidonoyl ethanolamide (AEA) in brain tissue and plasma in rats. PF-3845 has a Ki = 0.23 μM to the FAAH receptor. Various studies conclude that PF-3845 is an important pharmacological tool in determining the function of the endocannabinoid system.


References

1. Ahn, K., et al. 2009. Chem. Biol. 16: 411-420. PMID: 19389627
2. Long, J.Z., et al. 2011. J. Lipid Res. 52: 337-344. PMID: 21097653
3. Kinsey, S.G., et al. 2011. Pharmacol. Biochem. Behav. 98: 21-27. PMID: 21145341

Physical State :
Solid
Solubility :
Soluble in 1:3 EtOH;PBS(pH7.2) (~0.25 mg/ml), ethanol (~20 mg/ml), DMSO (~20 mg/ml), DMF (~20 mg/ml), and water (<1 mg/ml) at 25 °C.
Storage :
Store at -20° C
Ki Data :
FAAH: Ki= 0.23 µM
pK Values :
pKb: 5.70 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
25154867
SMILES :
C1CN(CCC1CC2=CC(=CC=C2)OC3=NC=C(C=C3)C(F)(F)F)C(=O)NC4=CN=CC=C4

Download SDS (MSDS)

Certificate of Analysis

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