LY2183240

Description

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LY2183240 is a highly potent blocker of anandamide uptake (IC₅₀= 270 pM; K_i=540 nM). LY2183240 is a potent, covalent inhibitor of the endocannabinoid-degrading enzyme fatty acid amide hydrolase (FAAH) with an IC₅₀ of 12.4 nM. LY2183240 inactivates FAAH by carbamylation of the enzyme’s serine nucleophile. LY2183240 also inhibits several other brain serine hydrolases with IC₅₀s of 5.3, 0.09, 8.2 nM for MAG lipase, bh6 and KIAA1363, respectively .

LY-2183240 is a potent, covalent inhibitor of the EC-degrading enzyme fatty acid amide hydrolase (FAAH). LY-2183240 disrupts the cellular uptake of the lipid endocannabinoid (EC) anandamide and promote analgesia in vivo. LY-2183240 is also an inhibitor of monoacylgylcerol lipase (MGL).

Technical Information
Formal Name
5-([1,1′-biphenyl]-4-ylmethyl)-N,N-dimethyl-1H-tetrazole-1-carboxamide
CAS Number
874902-19-9
Molecular Formula
C17H17N5O
Formula Weight
307.4
Purity
≥98%
Formulation
(Request formulation change)
A crystalline solid
Solubility
(Learn about Variance in Solubility)
DMF: 3 mg/ml
DMSO: 2 mg/ml
Ethanol: 10 mg/ml
Ethanol:PBS(pH 7.2) (1:5): 0.1 mg/ml
λmax
253 nm
SMILES
O=C(N(C)C)N1N=NN=C1CC2=CC=C(C3=CC=CC=C3)C=C2
InChi Code
InChI=1S/C17H17N5O/c1-21(2)17(23)22-16(18-19-20-22)12-13-8-10-15(11-9-13)14-6-4-3-5-7-14/h3-11H,12H2,1-2H3
InChi Key
GZNIYOXWFCDBBJ-UHFFFAOYSA-N

Shipping & Storage Information

Storage
-20°C
Shipping
Room Temperature in continental US; may vary elsewhere
Stability
≥ 2 years