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  3. Trimetazidine dihydrochloride

Trimetazidine dihydrochloride 

Cat. No.: HY-B0968 Purity: 99.96%
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Trimetazidine dihydrochloride is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC50 of 75 nM, which can inhibit β-oxidation of free fatty acid (FFA). Trimetazidine dihydrochloride is an effective antianginal agent and a cytoprotective drug, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties. Trimetazidine dihydrochloride triggers autophagy. Trimetazidine dihydrochloride is also a 3-hydroxyacyl-CoA dehydrogenase (HADHA) inhibitor.

For research use only. We do not sell to patients.

Trimetazidine dihydrochloride Chemical Structure

Trimetazidine dihydrochloride Chemical Structure

CAS No. : 13171-25-0

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10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
10 mg USD 60 In-stock
Estimated Time of Arrival: December 31
50 mg USD 96 In-stock
Estimated Time of Arrival: December 31
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Based on 2 publication(s) in Google Scholar

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Description

Trimetazidine dihydrochloride is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC50 of 75 nM, which can inhibit β-oxidation of free fatty acid (FFA). Trimetazidine dihydrochloride is an effective antianginal agent and a cytoprotective drug, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties. Trimetazidine dihydrochloride triggers autophagy. Trimetazidine dihydrochloride is also a 3-hydroxyacyl-CoA dehydrogenase (HADHA) inhibitor[1][2][3][4].

IC50 & Target

IC50: 75 nM (long chain 3-ketoyl coenzyme A thiolase)[2]
β-oxidation[2]
Autophagy[3]
3-hydroxyacyl-CoA dehydrogenase (HADHA)[4]

In Vitro

Trimetazidine (1 μM-100 μM; 24 hours; HUVECs) could enhance the viability of the injured HUVECs induces by oxidation in a certain dose-dependent manner[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: Human umbilical vein endothelial cells (HUVECs)
Concentration: 1 μM, 10 μM, 100 μM
Incubation Time: 24 hours
Result: Enhanced the viability of the injured HUVECs induced by oxidation.
In Vivo

Trimetazidine (5-20 mg/kg; oral administration; 1 hour; Swiss albino male mice) in 10 mg/kg and 20 mg/kg doses significantly raises the seizure-threshold current in the increasing current electroshock seizure (ICES) test in the mice[5].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Swiss albino male mice (24-35 g)[4]
Dosage: 5 mg/kg, 10 mg/kg and 20 mg/kg;
10 mL/kg body weight
Administration: Oral administration; 1 hour
Result: In 10 mg/kg and 20 mg/kg doses significantly raised the seizure-threshold current in the ICES test.
Clinical Trial
Molecular Weight

339.26

Formula

C₁₄H₂₄Cl₂N₂O₃

CAS No.

13171-25-0

SMILES

COC1=CC=C(CN2CCNCC2)C(OC)=C1OC.[H]Cl.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

H2O : ≥ 100 mg/mL (294.76 mM)

DMSO : 25 mg/mL (73.69 mM; Need ultrasonic)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9476 mL 14.7380 mL 29.4759 mL
5 mM 0.5895 mL 2.9476 mL 5.8952 mL
10 mM 0.2948 mL 1.4738 mL 2.9476 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (7.37 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (7.37 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

TrimetazidineAutophagyInhibitorinhibitorinhibit

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Product Name:
Trimetazidine dihydrochloride
Cat. No.:
HY-B0968
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