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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 |
| Formula | C17H17N5O |
| 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 |
|---|
| JNJ-1661010
JNJ-1661010 is a potent and selective FAAH inhibitor with IC50 of 10 nM (rat) and 12 nM (human), exhibits >100-fold selectivity for FAAH-1 when compared to FAAH-2. |
| URB597
URB597 is a potent, orally bioavailable FAAH inhibitor with IC50 of 4.6 nM, with no activity on other cannabinoid-related targets. |
| PF-3845
PF-3845 is a potent, selective and irreversible FAAH inhibitor with Ki of 230 nM, showing negligible activity against FAAH2. |
| Biochanin-A
Biochanin A is A naturally occurring fatty acid amide hydrolase (FAAH) inhibitor that inhibits FAAH in mice, rats and humans with FAAH IC50 of 1.8, 1.4 and 2.4 μM, respectively. |
| FAAH-IN-2
FAAH-IN-2 is a potent FAAH (fatty acid amide hydrolase) inhibitor. |
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