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PF-3845

Cat No.
CEI-1473
Description
PF-3845 is a selective inhibitor of fatty acid amide hydrolase (FAAH) with Ki value of 0.23 μM.
Product Overview
PF-3845 is a highly potent and selective inhibitor of fatty acid amide hydrolase (FAAH) with Ki value of 0.23μM. PF-3845 is a biaryl ether piperidine. It inhibits FAAH by a covalent, irreversible mechanism involving carbamylating FAAHs catalytic S241 nucleophile. It is found that, administration of PF-3845 to mice results a rapid and complete inactivation of FAAH in the brain. PF-3845 is highly selective for FAAH in vivo. It shows no activity to some other serine hydrolases as well as to a FAAH homologue, FAAH2.In addition, PF-3845-treated mice shows significant elevations in brain levels of AEA, other NAEs and liver levels of AEA, PEA and OEA. Moreover, PF-3845 is found to inhibit pain responses in a rat model of inflammatory pain. It is also found to reverse LPS-induced tactile allodynia in mice. This anti-allodynic effect requires activation of both CB1 and CB2 receptors which are the target receptors of the FAAH substrates.
CAS No.
1196109-52-0
Molecular Weight
456.46
Purity
0.98
Storage
Store at -20°C
Targets
FAAH
IC50
0.23 μM (Ki)
Molecular Formula
C24H23F3N4O2
Chemical Name
N-pyridin-3-yl-4-[[3-[5-(trifluoromethyl)pyridin-2-yl]oxyphenyl]methyl]piperidine-1-carboxamide
Solubility
Soluble in DMSO > 10 mM
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request
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