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当前位置: 首页 > 信号通路研究 > Hydroxylase > Mildronate
Mildronate
Mildronate
Mildronate
商品货号:CL-11096
CAS 号:76144-81-5
英文名字:Mildronate
质量标准:>98%
分子式:C6H14N2O2
  • 包装规格:
    规格 库存 发货时间
    50mg [¥1250.00]15 现货,一周内发货
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    商品信息

    质检证书(coa)

    说明书下载

     Mildronate

    分子式C6H14N2O2   分子量146.19

     

    产品描述

    Mildronate是一种γ-丁酰甜菜碱(GBB)羟化酶介导的L-肉碱生物合成的抑制剂并且可以作为肾脏肉毒碱重吸收的竞争性抑制剂。

    靶点

    HSP90

             

    IC50

    51 nM

             

    体外研究

    Mildronate (40 μM) inhibits the reaction of γ-butyrobetaine hydroxylase with γ-butyrobetaine with Km and Vmax of 36.8 μM and 0.08 nmol/min/mg protein, respectively.

    体内研究

    Mildronate administered orally to rats for 10 days (150 mg/kg) elicits a reduction in myocardial free camitine and long-chain acyl carnitine content by 63.7 and 74.3%, respectively. Mildronate treatment (100 mg/kg, orally) subsequent administration of isoproterenol results in a reduction in free camitine concentration by 48.7% in comparison with the rats receiving isoproterenol. A prior administration of Mildronate effectively protects the myocardium from isoproterenol-induced variations in the content of ATP and myocardial energy charge, as well as preventing a rise in creatine phosphokinase and lactic dehydrogenase activity. Mildronate (200 mg/kg) long-term treatment significantly increases the rate of insulin-stimulated glucose uptake by 35% and the expression of glucose transporter 4 (1.7-fold increase), hexokinase II (2.1-fold increase), insulin receptor proteins (2.5-fold increase) and carnitine palmitoyltransferases IA (2.2-fold increase) in mouse hearts. Mildronate long-term treatment statistically significantly decreases fed state blood glucose from 6 to 5 mM. Mildronate reduces the azidothymidine-induced alterations in mouse brain tissue. Mildronate (50 mg/kg) normalizes the increase in caspase-3, cellular apoptosis susceptibility protein (CAS) and iNOS expression. Mildronate also normalizes the changes in cytochromec oxidase (COX) expression, reduces the expression of glial fibrillary acidic protein (GFAP) and cellular infiltration. Mildronate displays protective effects in experimental model of type 2 diabetes in Goto-Kakizaki rats. Mildronate (200 mg/kg) treatment decreases both the fed- and fasted-state blood glucose. Mildronate strongly inhibits fructosamine accumulation and loss of pain sensitivity (by 75%) and also ameliorates the enhanced contractile responsiveness of Goto-Kakizaki rat aortic rings to phenylephrine. In addition, in Mildronate-treated hearts, the necrosis zone following coronary occlusion is significantly decreased by 30%.

    溶解性

    DMSO <1 mg/mL,水 29 mg/mL,乙醇 29 mg/mL

    稳定性

    2 -20°C粉状,6-80°C溶于DMSO

    特征

             

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