Fatty acid amide hydrolase (FAAH) is the enzyme responsible for hydrolysis and inactivation of fatty acid amides including anandamide and oleamide. CAY10435 is a selective, potent inhibitor of rat FAAH exhibiting a Ki value of 0.57 nM.1 Using a proteonomics approach, CAY10435 was screened against the serine hydrolase family of enzymes, of which FAAH is a member. In this assay, CAY10435 exhibited IC50 values of 0.81 nM, 83 nM, and 50 µM for FAAH, triacylglycerol hydrolase (TGH), and an uncharacterized hydrolase (KIAA1363), respectively.2 Knowledge of the specificity of CAY10435 obtained from this experiment should allow for more accurate interpretation of results using the inhibitor in complex environments such as whole cells or animals.
1
Boger, D.L., Sato, H., Lerner, A.E., et al. Exceptionally potent inhibitors of fatty acid amide hydrolase: The enzyme responsible for degradation of endogenous oleamide and anandamide. Proc Natl Acad Sci USA975044-5049(2000).
2
Leung, D., Hardouin, C., Boger, D.L., et al. Discovering potent and selective reversible inhibitors of enzymes in complex proteomes. Nat Biotech21(6)687-691(2003).
Formal Name
1-oxaxolo[4,5-b]pyridin-2-yl-1-dodecanone
CAS Number
288862-73-7
Molecular Formula
C18H26N2O2
Formula Weight
302.4
Formulation
A solution in methyl acetate
Purity
>98%
λmax
235, 296 nm
Stability
1 year
Storage
-20°C
Shipping
Room temperature
in continental US; may vary elsewhere
SMILES
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CCCCCCCCCCCC(=O)c1oc2cccnc2n1
Background Reading
Boger, D.L., Sato, H., Lerner, A.E., et al. Exceptionally potent inhibitors of fatty acid amide hydrolase: The enzyme responsible for degradation of endogenous oleamide and anandamide. Proc Natl Acad Sci USA975044-5049(2000).
Leung, D., Hardouin, C., Boger, D.L., et al. Discovering potent and selective reversible inhibitors of enzymes in complex proteomes. Nat Biotech21(6)687-691(2003).
CAY10435 is available in the following screening
library: