| 货号 | 15997-10mg |
| 描述 | Mildronate is a structural analog of γ-butyrobetaine (γBB), an intermediate in the biosynthesis of carnitine. It blocks carnitine synthesis by inhibiting γBB hydroxylase (IC50 = 62 µM) and, less potently, carnitine acetyltransferase (Ki = 1.6 mM).1,2,3 Through these actions, mildronate reduces the levels of free carnitine and long chain acyl carnitine.4,5 This leads to suppressed fatty acid metabolism and mitochondrial uncoupling during oxidative conditions, resulting in cardioprotective and neuroprotective effects.4,5,6 Mildronate also improves cognition and reduces amyloid-β pathology in a mouse model of Alzheimer’s disease.7 |
| 别名 | Meldonium;MET-88;Quaterine;THP; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Tars, K.,Leitans, J.,Kazaks, A., et al. Targeting carnitine biosynthesis: Discovery of new inhibitors against γ-butyrβne hydroxylase. Journal of Medicinal Chemistry 57(6), 2213-2236 (2014). 2.Leung, I.K.,Krojer, T.J.,Kochan, G.T., et al. Structural and mechanistic studies on γ-butyrβne hydroxylase. Chemistry & Biology 17(12), 1316-1324 (2010). 3.Jaudzems, K.,Kuka, J.,Gutsaits, A., et al. Inhibition of carnitine acetyltransferase by mildronate, a regulator of energy metabolism. Journal of Enzyme Inhibition and Medicinal Chemistry 24(6), 1269-1275 (2009). 4.Simkhovich, B.Z.,Shutenko, Z.V.,Meirena, D.V., et al. 3-(2,2,2-Trimethylhydrazinium)propionate (THP)--a novel γ-butyrβne hydroxylase inhibitor with cardioprotective properties. Biochemical Pharmacology 37(2), 195-202 (1988). 5.Makrecka, M.,Svalbe, B.,Volska, K., et al. Mildronate, the inhibitor of L-carnitine transport, induces brain mitochondrial uncoupling and protects against anoxia-reoxygenation. European Journal of Pharmacology 723, 55-61 (2014). 6.Klusa, V.,Beitnere, U.,Pupure, J., et al. Mildronate and its neuroregulatory mechanisms: Targeting the mitochondria, neuroinflammation, and protein expression. Medicina (Kaunas) 49(7), 301-309 (2013). 7.Beitnere, U.,van Groen, T.,Kumar, A., et al. Mildronate improves cognition and reduces amyloid-β pathology in transgenic Alzheimer’s disease mice. Journal of Neuroscience Research 92(3), 338-346 (2014). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 182.2 |
| 分子式 | C6H14N2O2 • 2H2O |
| CAS号 | 86426-17-7 |
| 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。 |