| 货号 | 15600-50mg |
| 描述 | Thiorphan is a potent inhibitor of neprilysin, a membrane metallo-endopeptidase that cleaves peptide hormones, such as enkephalins, glucagon, and bradykinin (Ki = 4-140 nM).1,2,3 It is much less effective against neprilysin-2 (IC50 = 22.1 μM), angiotensin-converting enzyme, and endothelin-converting enzyme-1.4,1,2,3 Thiorphan can be produced in vivovia the metabolism of the prodrug acetorphan.5 Neprilysin is overexpressed in many forms of cancer and may play a role in protecting against Alzheimer’s disease. |
| 别名 | DL-Thiorphan; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Inguimbert, N.,Coric, P.,Poras, H., et al. Toward an optimal joint recognition of the S1 subsites of endothelin converting enzyme-1 (ECE-1), angiotensin converting enzyme (ACE), and neutral endopeptidase (NEP). Journal of Medicinal Chemistry 45(7), 1477-1486 (2002). 2.Elliott, R.L.,Marks, N.,Berg, M.J., et al. Synthesis and biological evaluation of phosphonamidate peptide inhibitors of enkephalinase and angiotensin-converting enzyme. Journal of Medicinal Chemistry 28(9), 1208-1216 (1985). 3.Gomez-Monterrey, I.,Turcaud, S.,Lucas, E., et al. Exploration of neutral endopeptidase active site by a series of new thiol-containing inhibitors. Journal of Medicinal Chemistry 36(1), 87-94 (1993). 4.Whyteside, A.R. and Turner, A.J. Human neprilysin-2 (NEP2) and NEP display distinct subcellular localisations and substrate preferences. FEBS Letters 582(16), 2382-2386 (2008). 5.Spillantini, M.,Gepetti, P.,Fanciullacci, M., et al. In vivo “enkephalinase” inhibition by acetorphan in human plasma and CSF. European Journal of Pharmacology 125(1), 147-150 (1986). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥95% |
| 计算分子量 | 253.3 |
| 分子式 | C12H15NO3S |
| CAS号 | 76721-89-6 |
| 稳定性 | ≥ 2 years |
| 本官网所有报价均为常温或者蓝冰运输价格，如有产品需要干冰运输，需另外加收干冰运输费。 |