Choose Your Country or Region

Mildronate

Name: Mildronate
Brand: Selleck Chemicals
SKU: S4130
Rating: 5 (1 reviews)

Catalog No.S4130 Synonyms: Meldonium, MET-88, Quaterin

For research use only.

Mildronate (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.

CAS No. 76144-81-5

Selleck's Mildronate has been cited by 1 Publication

Purity & Quality Control

Choose Selective Hydroxylase Inhibitors

Related Compound Libraries

Other Hydroxylase Products

U73122^New

U73122 is a potent phospholipase C (PLC) inhibitor, which reduces agonist-induced Ca²⁺ increases in platelets and PMN. U73122 potently inhibits human 5-lipoxygenase (5-LO).
Liproxstatin-1^New

Liproxstatin-1 is a potent ferroptosis inhibitor with an IC50 of 22 nM.
Epacadostat (INCB024360)^New

Epacadostat (INCB024360) is a potent and selective indoleamine 2,3-dioxygenase (IDO1) inhibitor with IC50 of 10 nM and displays high selectivity over other related enzymes such as IDO2 or tryptophan 2,3-dioxygenase (TDO).
Isotretinoin

Isotretinoin (13-cis retinoic acid) was developed to be used as a chemotherapy medication for the treatment of brain cancer, pancreatic cancer and more.
Telotristat Etiprate (LX 1606 Hippurate)

Telotristat Etiprate (LX 1606 Hippurate) is an orally bioavailable, tryptophan hydroxylase (TPH) inhibitor with potential antiserotonergic activity. Phase 3.
Tetrahydropapaverine HCl

Tetrahydropapaverine (Norlaudanosine), one of the TIQs and an analogue of salsolinol and tetrahydropapaveroline, has been reported to have neurotoxic effects on dopamine neurons.
Nepicastat (SYN-117) HCl

Nepicastat (SYN-117) HCl is a potent and selective inhibitor of both bovine and human dopamine-β-hydroxylase with IC50 of 8.5 nM and 9 nM, with negligible affinity for twelve other enzymes and thirteen neurotransmitter receptors. Phase 2.
(R)-Nepicastat HCl

(R)-Nepicastat HCl (RS-25560-198), the R-enantiomer of Nepicastat HCl, is a potent and selective inhibitor with IC50 of 25.1 nM and 18.3 nM for bovine and human dopamine-β-hydroxylase, with negligible affinity for twelve other enzymes and thirteen neurotransmitter receptors.
DMOG

DMOG (Dimethyloxalylglycine) is an antagonist of α-ketoglutarate cofactor and inhibitor for HIF prolylhydroxylase, leading to stabilisation and accumulation of HIF-1α protein in the nucleus. DMOG enhances autophagy.
Erastin

Erastin is a ferroptosis activator by acting on mitochondrial VDAC, exhibiting selectivity for tumor cells bearing oncogenic RAS. Solutions of Erastin are best fresh-prepared.

Download Inhibitor Catalog

Hydroxylase Signaling Pathway Map

Biological Activity

Description

Mildronate (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

Mildronate (40 μM) inhibits the reaction of γ-butyrobetaine hydroxylase with γ-butyrobetaine with K_m and V_max 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] 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%. ^[4]

Protocol (from reference)

References

[4] Liepinsh E, et al. Br J Pharmacol, 2009, 157(8), 1549-1556.

+ Expand

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight	147.19
Formula	C₆H₁₄N₂O₂
CAS No.	76144-81-5
Storage	3 years	-20°C	powder
Storage	2 years	-80°C	in solvent
Smiles	C[N+](C)(C)NCCC(=O)[O-].O.O

Download Mildronate SDF

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

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

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):