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Mildronate dihydrate

Mildronate dihydrate
Mildronate dihydrate is an inhibitor of biosynthesis of L-carnitine by gamma-butyrobetaine (GBB) hydroxylase and as a competitive inhibitor of renal carnitine reabsorption.
Catalog No. T6586Cas No. 86426-17-7
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Mildronate dihydrate

Catalog No. T6586Alias Mildronate, MeldoniumCas No. 86426-17-7

Mildronate dihydrate is an inhibitor of biosynthesis of L-carnitine by gamma-butyrobetaine (GBB) hydroxylase and as a competitive inhibitor of renal carnitine reabsorption.
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Pack SizePriceAvailabilityQuantity
25 mg$38In Stock
50 mg$56In Stock
100 mg$81In Stock
500 mg$197In Stock
1 mL x 10 mM (in H2O)$29In Stock
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Product Introduction

Bioactivity
Description
Mildronate dihydrate is an inhibitor of biosynthesis of L-carnitine by gamma-butyrobetaine (GBB) hydroxylase and as a competitive inhibitor of renal carnitine reabsorption.
Targets&IC50
BBOX (human recombinant):34-62 μM (IC50), OCTN2 (human):21 μM (EC50)
In vitro
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. [1]
In vivo
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. [1] 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. [2] 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. [3]
AliasMildronate, Meldonium
Chemical Properties
Molecular Weight182.22
FormulaC6H18N2O4
Cas No.86426-17-7
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: Insoluble
H2O: 10 mM
Solution Preparation Table
H2O
1mg5mg10mg50mg
1 mM5.4879 mL27.4394 mL54.8787 mL274.3936 mL
5 mM1.0976 mL5.4879 mL10.9757 mL54.8787 mL
10 mM0.5488 mL2.7439 mL5.4879 mL27.4394 mL

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