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LY2183240

Anandamide transporter inhibitor
 
BML-CR113-0010 10 mg 72.00 USD
 
BML-CR113-0050 50 mg 296.00 USD
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Replaces Prod. #: ALX-550-411

A potent inhibitor of anandamide uptake (IC50=7.3nM). Systemic administration to rodents elevates brain anandamide levels and shows efficacy in a rodent model of persistent pain. LY2183240 also inhibits FAAH hydrolytic activity (IC50=12.4nM) as well as other brain serine proteases and represents a new chemotype for the design of new selective FAAH inhibitors. Radiolabeled LY2183240 has been used to identify a high-affinity, saturable anandamide transporter binding site on RBL-2H3 cell membranes distinct from FAAH.

Product Specification

Alternative Name:5-Biphenyl-4-ylmethyl-tetrazole-1-carboxylic acid dimethylamide
 
Formula:C17H17N5O
 
MW:307.4
 
CAS:874902-19-9
 
Purity:≥98% (TLC)
 
Identity:Determined by NMR.
 
Appearance:White to off-white solid.
 
Solubility:Soluble in DMSO (>25mg/ml), 100% ethanol (12mg/ml) or dimethyl formamide.
 
Shipping:Ambient
 
Long Term Storage:-20°C
 
Use/Stability:Store as supplied, at -20°C for up to 1 year. Store solutions at -20°C for up to 3 months.
 
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Product Literature References

Carbamoyl tetrazoles as inhibitors of endocannabinoid inactivation: a critical revisitation: G. Ortar et al.; Eur. J. Med. Chem. 43, 62 (2008), Abstract;
Pharmacological characterization of endocannabinoid transport and fatty acid amide hydrolase inhibitors: A.K. Dickason-Chesterfield et al.; Cell. Mol. Neurobiol. 26, 407 (2006), Abstract;
The putative endocannabinoid transport blocker LY2183240 is a potent inhibitor of FAAH and several other brain serine hydrolases: J.P. Alexander & B.F. Cravatt; J. Am. Chem. Soc. 128, 9699 (2006), Abstract;
Identification of a high-affinity binding site involved in the transport of endocannabinoids: S.A. Moore et al.; PNAS 102, 17852 (2005), Abstract;
Toward an anandamide transporter: R. Mechoulam & D.G. Deutsch; PNAS 102, 17541 (2005), Abstract;

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Anandamide transporter
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