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 Details
| Alternative Name: | 5-Biphenyl-4-ylmethyl-tetrazole-1-carboxylic acid dimethylamide |
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| Formula: | C17H17N5O |
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| MW: | 307.4 |
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| CAS: | 874902-19-9 |
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| Purity: | ≥98% (TLC) |
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| Identity: | Determined by NMR. |
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| Appearance: | White to off-white solid. |
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| Solubility: | Soluble in DMSO (>25mg/ml), 100% ethanol (12mg/ml) or dimethyl formamide. |
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| Shipping: | Ambient Temperature |
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| Long Term Storage: | -20°C |
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| 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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| Regulatory Status: | RUO - Research Use Only |
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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;
