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LY2183240 is a highly potent blocker of anandamide uptake (IC50= 270 pM; Ki=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 .
| Molecular Weight | 307.35 |
| CAS Number | 874902-19-9 |
| Solubility (25°C) | DMSO 50 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[4] Ya Fatou Njie, et al. Aqueous humor outflow effects of 2-arachidonylglycerol
| Related FAAH Products |
|---|
| JP104
JP104, a aryl carbamate, is an irreversible FAAH inhibitor with a pIC50 of ~8. |
| AM1172
AM1172 is metabolically stable anandamide uptake inhibitor and FAAH inhibitor. |
| URB937
URB937 is an orally active and peripherally restricted FAAH inhibitor (IC50=26.8 nM) and increases anandamide levels. |
| JNJ-40355003
JNJ-40355003 is a potent and selective atty acid amide hydrolase (FAAH) inhibitor. |
| N-Benzyllinolenamide
N-Benzyllinolenamide is a natural macamide isolated from Lepidium meyenii, acts as an inhibitor of fatty acid amide hydrolase (FAAH) with an IC50 of 41.8 μM. |
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