Home Metabolism Hydroxylase inhibitor Meldonium For research use only.

Meldonium

Synonyms: MET-88, Quaterin

Meldonium (MET-88, Quaterin) is an inhibitor of biosynthesis of L-carnitine by gamma-butyrobetaine (GBB) hydroxylase and as a competitive inhibitor of renal carnitine reabsorption.

Meldonium Chemical Structure

Meldonium Chemical Structure

CAS: 76144-81-5

Selleck's Meldonium has been cited by 3 publications

Purity & Quality Control

Batch: Purity: 100.00%
100.0

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Biological Activity

Description Meldonium (MET-88, Quaterin) is an inhibitor of biosynthesis of L-carnitine by gamma-butyrobetaine (GBB) hydroxylase and as a competitive inhibitor of renal carnitine reabsorption.
Targets
GBB hydroxylase [1]
In vitro
In vitro

Meldonium (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
In vivo

Meldonium 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. Meldonium 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 Meldonium 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] Meldonium  (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. Meldonium long-term treatment statistically significantly decreases fed state blood glucose from 6 to 5 mM. [2] Meldonium reduces the azidothymidine-induced alterations in mouse brain tissue. Meldonium (50 mg/kg) normalizes the increase in caspase-3, cellular apoptosis susceptibility protein (CAS) and iNOS expression. Meldonium also normalizes the changes in cytochromec oxidase (COX) expression, reduces the expression of glial fibrillary acidic protein (GFAP) and cellular infiltration. [3] Meldonium displays protective effects in experimental model of type 2 diabetes in Goto-Kakizaki rats. Meldonium (200 mg/kg) treatment decreases both the fed- and fasted-state blood glucose. Meldonium 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 Meldonium-treated hearts, the necrosis zone following coronary occlusion is significantly decreased by 30%. [4]

Chemical lnformation & Solubility

Molecular Weight 147.19 Formula

C6H14N2O2
CAS No. 76144-81-5 SDF Download Meldonium SDF
Smiles C[N+](C)(C)NCCC(=O)[O-].O.O
Storage (From the date of receipt)

In vitro
Batch:

Water : 29 mg/mL

Ethanol : 29 mg/mL

DMSO : Insoluble ( Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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