| Identification | Back Directory | [Name]
2H-Tetrazole-2-carboxaMide, 5-([1,1'-biphenyl]-4-ylMethyl)-N,N-diMethyl- | [CAS]
1010096-65-7 | [Synonyms]
LY2183240 2&rsquo
LY2183240 2’-isomer
LY2183240 2'-isomer Exclusive
5-([1,1-biphenyl]-4-ylmethyl)-N,N-dimethyl-2H-tetrazole-2-carboxamide
2H-Tetrazole-2-carboxaMide, 5-([1,1'-biphenyl]-4-ylMethyl)-N,N-diMethyl- | [Molecular Formula]
C17H17N5O | [MOL File]
1010096-65-7.mol | [Molecular Weight]
307.35 |
| Chemical Properties | Back Directory | [Boiling point ]
506.1±53.0 °C(Predicted) | [density ]
1.21±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMF: 3 mg/ml; DMSO: 2 mg/ml; Ethanol: 10 mg/ml; Ethanol:PBS(pH 7.2) (1:5): 0.1 mg/ml | [form ]
A crystalline solid | [pka]
-1.73±0.12(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Description]
LY2183240 is a potent, competitive small molecule inhibitor of anandamide uptake (IC50 = 270 pM; Ki = 540 pM) and hydrolysis. It has been shown to increase anandamide levels in rat cerebellum (ED50 = 1.37 mg/kg) and displays dose-dependent efficacy (3-30 mg/kg) in several rodent models of persistent pain. LY2183240 2’-isomer is a less potent, 2,5-regioisomer of LY2183240 that inhibits anandamide hydrolysis and uptake with IC50 values of 33 and 998 nM, respectively. | [Uses]
5-([1,1''-Biphenyl]-4-ylmethyl)-N,N-dimethyl-2H-tetrazole-2-carboxamide is an inhibitor of human monoacylglycerol lipase (hMGL). | [storage]
Store at -20°C | [References]
[1] S A MOORE. Identification of a high-affinity binding site involved in the transport of endocannabinoids.[J]. Proceedings of the National Academy of Sciences of the United States of America, 2005, 102 49: 17852-17857. DOI: 10.1073/pnas.0507470102
[2] GIORGIO ORTAR . Carbamoyl tetrazoles as inhibitors of endocannabinoid inactivation: A critical revisitation[J]. European Journal of Medicinal Chemistry, 2008, 43 1: Pages 62-72. DOI: 10.1016/j.ejmech.2007.02.023
[3] MARZO V D. Targeting the endocannabinoid system: to enhance or reduce?[J]. Nature Reviews. Drug Discovery, 2008, 7 5: 438-455. DOI: 10.1038/nrd2553 |
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