LY-2183240 (874902-19-9) is highly potent inhibitor of cellular anandamide uptake (IC50 = 0.27nM1, 15nM2). LY-2183240 has also been found2-4 to be an inhibitor of fatty acid amide hydrolase (FAAH) – IC50 = 14nM4, diacylglycerol lipase (DAGL) and monoacylglycerol lipase (MAGL) – IC50 = 5.3 nM3. anandamidly -2183240(874902-19-9)是细胞吸收anandamide的高效抑制剂(IC50 = 0.27nM1, 15nM2)。 LY-2183240还被发现是脂肪酸酰胺水解酶(FAAH) - IC50 = 14nM4、二酰基甘油脂肪酶(DAGL)和单酰基甘油脂肪酶(MAGL) - IC50 = 5.3 nM3的抑制剂。
References/Citations:
1) Moore et al., (2005), Identification of a high-affinity binding site involved in the transport of endocannabinoids; Proc. Natl. Acad. Sci. USA, 102 17852 2) Ortar et al. (2008), Carbamoyl tetrazoles as inhibitors of endocannabinoid inactivation: A critical revision; Eur. .J. Med. Chem., 43 62 3) Alexander and Cravatt (2006), The putative endocannabinoid transport blocker LY2183240 is a potent inhibitor of FAAH and several other brain serine hydrolases; J. Am. Chem. Soc., 128 9699 4) Dickason-Chesterfield et al. (2006), Pharmacological Characterization of Endocannabinoid Transport and Fatty Acid Amide Hydrolase Inhibitors; Cell. Mol. Neurobiol., 26 405
CAS:
874902-19-9
Catalog Number:
10-2636
Activity:
Andamide uptake inhibitor
Chemical Name:
5-([1,1′-Biphenyl]-4-ylmethyl)-N,N,-dimethyl-1H-tetrazole-1-carboxamide
Molecular Weight:
307.35
Molecular Formula:
C17H17N5O
Solubility:
Soluble in DMSO (greater than 25 mg/ml) or in Ethanol (up to 15 mg/ml).
Physical Properties:
White solid
Purity:
98%
NMR (Conforms)
Storage Temperature:
-20°
Stability:
Stable for 1 year as supplied. Solutions in DMSO of ethanol may be stored at -20°C for up to 1 month
Shipping Code:
RT
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