1. Metabolic Enzyme/Protease
    Neuronal Signaling
    Autophagy
  2. FAAH
    Autophagy
  3. LY2183240

LY2183240 

Cat. No.: HY-10865 Purity: 99.07%
Handling Instructions

LY2183240 is a highly potent blocker of anandamide uptake (IC50= 270 pM; Ki=540 nM). LY2183240 is a potent, covalent inhibitor of the EC-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 .

For research use only. We do not sell to patients.

LY2183240 Chemical Structure

LY2183240 Chemical Structure

CAS No. : 874902-19-9

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 88 In-stock
Estimated Time of Arrival: December 31
10 mg USD 80 In-stock
Estimated Time of Arrival: December 31
50 mg USD 330 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

LY2183240 is a highly potent blocker of anandamide uptake (IC50= 270 pM; Ki=540 nM). LY2183240 is a potent, covalent inhibitor of the EC-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[1][2] [3].

In Vivo

LY2183240 (3-30mg/kg; i.p.) dose-dependently attenuates formalin-induced paw-licking pain behavior in the formalin model of persistent pain mechanisms[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Sprague-Dawley rats (Formalin Pain Model)[1]
Dosage: 3, 10, 30 mg/kg
Administration: I.p.
Result: Dose-dependently attenuated formalin-induced paw-licking pain behavior in the formalin model of persistent pain mechanisms.
Molecular Weight

307.35

Formula

C₁₇H₁₇N₅O

CAS No.

874902-19-9

SMILES

O=C(N(C)C)N1N=NN=C1CC(C=C2)=CC=C2C3=CC=CC=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (162.68 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.2536 mL 16.2681 mL 32.5362 mL
5 mM 0.6507 mL 3.2536 mL 6.5072 mL
10 mM 0.3254 mL 1.6268 mL 3.2536 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (8.13 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (8.13 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

LY2183240LY 2183240LY-2183240FAAHAutophagyFatty acid amide hydrolaseanandamideuptaketransportbrainserinehydrolasesInhibitorinhibitorinhibit

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Product Name:
LY2183240
Cat. No.:
HY-10865
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