LY-2183240

For research use only.

Catalog No.S8052

LY-2183240 Chemical Structure

CAS No. 874902-19-9

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).

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Biological Activity

Description 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).
Targets
FAAH [1]
()
MGL [2]
()
In vitro

LY2183240 inhibits anandamide uptake in live cell with IC50 of 0.27 nM. [1] LY2183240 inactivates FAAH by carbamylation of the enzyme’s serine nucleophile. LY2183240 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. [2]

In vivo

LY2183240 (i.p.) results in a dose-dependent increase in anandamide concentrations in rat cerebellum with ED50 of 1.37 mg/kg. LY2183240 (i.p.) dose-dependently attenuates formalin-induced paw-licking pain behavior in the formalin model of persistent pain mechanisms. [1] LY2183240 (10 mg/kg, i.p.) treatment for 90 min inactivates FAAH (100% inhibited), Abh6 (>90% inhibited), and MAG lipase (>60% inhibited) in brain tissue. [2] LY2183240 shows beneficiation on fear-potentiated startle (FPS) and alcohol-seeking behaviors (HAP) in mice selectively bred for high alcohol preference. Repeated administration of LY2183240 (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 LY2183240 enhances the expression of alcohol-induced conditioned place preference and this effect persisted in the absence of the drug. [3]

Protocol

Cell Research:

[2]

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  • Cell lines: mouse brain membranes
  • Concentrations: 0.001-10 μM
  • Incubation Time: 10 min
  • Method:

    FAAH activity is measured in mouse brain membranes in the presence of varying concentrations of inhibitor. Brain membranes (1 mg/mL) from FAAH (-/-) mice are used as a control. Briefly, varying concentrations of LY2183240 (1 μL, 100×stock in DMSO added to provide 0.001-10 μM final concentration) are preincubated with brain membranes (1 mg/mL in 50 mM Tris, pH 8, 94 μL) for 10 min.


    (Only for Reference)
Animal Research:

[2]

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  • Animal Models: male wild type or FAAH (-/-) C57Bl/6 mice
  • Dosages: 10 mg/kg
  • Administration: IP
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 61 mg/mL (198.47 mM)
Water Insoluble
Ethanol '''61 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 307.35
Formula

C17H17N5O

CAS No. 874902-19-9
Storage 2 years -80 in solvent
Synonyms N/A

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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FAAH Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID