Home Metabolism FAAH inhibitor LY-2183240

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LY-2183240 FAAH inhibitor

Cat.No.S8052

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

Chemical Structure

Molecular Weight: 307.35

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Quality Control

Batch: Purity: 99.01%
99.01

Solubility

In vitro
Batch:

DMSO : 61 mg/mL (198.47 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 61 mg/mL

Water : Insoluble

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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight 307.35 Formula

C17H17N5O

 Storage (From the date of receipt) 3 years-21°C powder
CAS No. 874902-19-9 -- Storage of Stock Solutions

Synonyms N/A Smiles CN(C)C(=O)[N]1N=NN=C1CC2=CC=C(C=C2)C3=CC=CC=C3

Mechanism of Action

Targets/IC50/Ki
FAAH
MGL
In vitro

LY2183240 inhibits anandamide uptake in live cell with IC50 of 0.27 nM. This compound inactivates FAAH by carbamylation of the enzyme’s serine nucleophile. It also inhibits KIAA1363, α/β-hydrolase 6 (Abh6) and monoacylglycerol lipase (MAG lipase) expressed in COS-7 cells with IC50 of 8.3, 0.09 and 5.3 nM, respectively.

In vivo

LY2183240 (i.p.) results in a dose-dependent increase in anandamide concentrations in rat cerebellum with ED50 of 1.37 mg/kg. This compound (i.p.) dose-dependently attenuates formalin-induced paw-licking pain behavior in the formalin model of persistent pain mechanisms. This chemical (10 mg/kg, i.p.) treatment for 90 min inactivates FAAH (100% inhibited), Abh6 (>90% inhibited), and MAG lipase (>60% inhibited) in brain tissue. It shows beneficiation on fear-potentiated startle (FPS) and alcohol-seeking behaviors (HAP) in mice selectively bred for high alcohol preference. Repeated administration of this compound (30 mg/kg) reduces the expression of FPS in HAP mice when given prior to a second FPS test 48 h after fear conditioning. Both the 10 and 30 mg/kg doses of this chemical enhances the expression of alcohol-induced conditioned place preference and this effect persisted in the absence of the drug.

References
  • [4] https://pubmed.ncbi.nlm.nih.gov/18597752/

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