- LY2183240 powder
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- $29.00 / 1KG
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2021-11-15
- CAS:874902-19-9
- Min. Order: 1KG
- Purity: 99%
- Supply Ability: 500ton/Month
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| | 5-[[(1,1'-BIPHENYL)-4-YL]METHYL]-N,N-DIMETHYL-1H-TETRAZOLE-1-CARBOXAMIDE Basic information |
| Product Name: | 5-[[(1,1'-BIPHENYL)-4-YL]METHYL]-N,N-DIMETHYL-1H-TETRAZOLE-1-CARBOXAMIDE | | Synonyms: | 5-[[(1,1'-BIPHENYL)-4-YL]METHYL]-N,N-DIMETHYL-1H-TETRAZOLE-1-CARBOXAMIDE;LY 2183240;LY-2183240 MN-25;1H-Tetrazole-1-carboxamide, 5-([1,1′-biphenyl]-4-ylmethyl)-N,N-dimethyl-;5-Biphenyl-4-ylmethyl-tetrazole-1-carboxylic acid dimethylamide;N,N-dimethyl-5-[(4-phenylphenyl)methyl]tetrazole-1-carboxamide;5-(biphenyl-4-ylMethyl)-N,N-diMethyl-1H-tetrazole-1-carboxaMide;LY2183240/LY-2183240 | | CAS: | 874902-19-9 | | MF: | C17H17N5O | | MW: | 307.35 | | EINECS: | | | Product Categories: | | | Mol File: | 874902-19-9.mol | ![5-[[(1,1'-BIPHENYL)-4-YL]METHYL]-N,N-DIMETHYL-1H-TETRAZOLE-1-CARBOXAMIDE Structure](CAS/GIF/874902-19-9.gif) |
| | 5-[[(1,1'-BIPHENYL)-4-YL]METHYL]-N,N-DIMETHYL-1H-TETRAZOLE-1-CARBOXAMIDE Chemical Properties |
| Melting point | 87-88℃ | | Boiling point | 506.1±53.0 °C(Predicted) | | density | 1.21 | | storage temp. | Sealed in dry,2-8°C | | solubility | Soluble in DMSO (greater than 25 mg/ml) or in Ethanol (up to 15 mg/ml). | | pka | 0.01±0.10(Predicted) | | form | White to off-white solid. | | color | White | | Stability: | Stable for 1 year as supplied. Solutions in DMSO of ethanol may be stored at -20°C for up to 1 month |
| Hazard Codes | Xn | | Risk Statements | 22 |
| | 5-[[(1,1'-BIPHENYL)-4-YL]METHYL]-N,N-DIMETHYL-1H-TETRAZOLE-1-CARBOXAMIDE Usage And Synthesis |
| Description | 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. | | Uses | LY2183240 is a potent inhibitor of FAAH activity, and the uptake and enzymatic hydrolysis of anandamide. Synthetic Cannabinoids | | Definition | ChEBI: N,N-dimethyl-5-[(4-phenylphenyl)methyl]-1-tetrazolecarboxamide is a member of biphenyls. | | Biological Activity | Novel and highly potent blocker of anandamide uptake (IC 50 = 270 pM). Inhibits fatty acid amide hydrolase (FAAH) activity (IC 50 = 12.4 nM). Following i.p. administration in rats, increases brain anandamide concentration and exerts antinociceptive effects in formalin model of pain. | | in vivo | LY2183240 (3-30mg/kg; i.p.) dose-dependently attenuates formalin-induced paw-licking pain behavior in the formalin model of persistent pain mechanisms[1]. | Animal Model: | Male Sprague-Dawley rats (Formalin Pain Model)[1] | | Dosage: | 3, 10, 30 mg/kg | | Administration: | I.p. | | Result: | Dose-dependently attenuated formalin-induced paw-licking pain behavior in the formalin model of persistent pain mechanisms.
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| | 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] JESSICA P. ALEXANDER Benjamin F C. The Putative Endocannabinoid Transport Blocker LY2183240 Is a Potent Inhibitor of FAAH and Several Other Brain Serine Hydrolases[J]. Journal of the American Chemical Society, 2006, 128 30: 9699-9704. DOI:10.1021/ja062999h
[4] AMY K DICKASON-CHESTERFIELD. Pharmacological characterization of endocannabinoid transport and fatty acid amide hydrolase inhibitors.[J]. Cellular and Molecular Neurobiology, 2006, 26 4-6: 407-423. DOI:10.1007/s10571-006-9072-6 |
| | 5-[[(1,1'-BIPHENYL)-4-YL]METHYL]-N,N-DIMETHYL-1H-TETRAZOLE-1-CARBOXAMIDE Preparation Products And Raw materials |
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