Meldonium dihydrate
产品说明书
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同义名 : | MET-88 dihydrate; Quaterin dihydrate; THP; Quaterine; MET-88; Meldonium; Mildronate(hydrate); Meldonium(dihydrate) |
| CAS号 : | 86426-17-7 | |
| 货号 : | A244186 | |
| 分子式 : | C6H18N2O4 | |
| 纯度 : | 98% | |
| 分子量 : | 182.22 | |
| MDL号 : | MFCD13461779 | |
| 存储条件： |
Pure form Inert atmosphere, 2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 4 mg/mL(21.95 mM)，配合低频超声，水浴加热至45℃，并调节pH至4，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO H2O: 100 mg/mL(548.79 mM)，配合低频超声助溶 |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | γ-butylbetaine (GBB) hydroxylase catalyses the hydroxylation of γ-butyrobetaine to carnitine. This is the final step in the biosynthesis of L-carnitine from 6-N-trimethyl-L-lysine. Mildronate is an inhibitor of L-carnitine biosynthetic mediated by γ-butylbetaine (GBB) hydroxylase, and can be a competitive inhibitor of carnitine reabsorption in the kidney[3]. In vitro, Mildronate (40 μM) inhibited the reaction between γ-butyryl betaine hydroxylase and γ-butyryl betaine, and the Km and Vmax values were 36.8 μM and 0.08 nmol/min/mg proteins, respectively[3]. In vivo，Mildronate reduced the levels of free carnitine and long-chain acyl carnitine in myocardium by 63.7% and 74.3%, respectively, in rats after 10 days of oral administration (150 mg/kg). When treated with Mildronate (100 mg/kg, oral), the concentration of free carnitine decreased by 48.7% compared with the rats only treated with isoproterenol. Priority administration of Mildronate can effectively protect the myocardium from damage caused by isoproterenol-induced changes in ATP content and myocardial energy charge, and also prevent the increase of creatine phosphokinase and lactate dehydrogenase activity[3]. In mouse hearts, long-term treatment with Mildronate (200 mg/kg) significantly increased insulin stimulated glucose uptake by 35%, and increased the expression of glucose transporter IV(1.7-fold increase), hexokinase II (2.1-fold increase), insulin receptor protein (2.5-fold increase) and carnitine palmityl transferase IA (2.2-fold increase). Long-term treatment with Mildronate has statistically significantly reduced the blood glucose level in the supply state from 6 mM to 5 mM[4]. Mildronate has a protective effect on type 2 diabetes in rats with Goto-Kakizaki. Treatment with Mildronate (200mg/kg) also lowers the blood sugar level during feeding and fasting. Mildronate strongly inhibited the accumulation of fructosamine and the loss of pain sensitivity (by 75%), and also improved the increased systolic response of the aortic ring to phenylephrine in rats with Goto-Kakizaki. In addition, in the heart treated with Mildronate, the necrotic area of myocardial infarction was significantly reduced by 30%[5]. | ||
| 实验方案 | |||
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| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
5.49mL 1.10mL 0.55mL |
27.44mL 5.49mL 2.74mL |
54.88mL 10.98mL 5.49mL |
| 参考文献 |
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