2. Autophagy
  3. Autophagy
  4. Trimetazidine

Trimetazidine 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 is an effective antianginal agent and a cytoprotective agent, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties. Trimetazidine triggers autophagy. Trimetazidine is also a 3-hydroxyacyl-CoA dehydrogenase (HADHA) inhibitor.

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

Trimetazidine Chemical Structure

Trimetazidine Chemical Structure

CAS No. : 5011-34-7

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5 mg USD 38 In-stock
10 mg USD 60 In-stock
50 mg USD 96 In-stock
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Based on 5 publication(s) in Google Scholar

Other Forms of Trimetazidine:

Trimetazidine Related Antibodies

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  • Biological Activity

  • Purity & Documentation

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Description

Trimetazidine 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 is an effective antianginal agent and a cytoprotective agent, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties. Trimetazidine triggers autophagy. Trimetazidine 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 (1-100 μM; 24 hours; HUVECs) could enhance the viability of the injured HUVECs induced by oxidation in a certain dose-dependent manner[1].

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

Trimetazidine Related Antibodies

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 and 20mg/kg doses significantly raises the seizure-threshold current in the ICES test in the mice[5].

MedChemExpress (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 and 20mg/kg doses significantly raised the seizure-threshold current in the ICES test.
Clinical Trial
Molecular Weight

266.34

Formula

C14H22N2O3
CAS No.
Appearance

Oil

Color

White to off-white

SMILES

COC1=CC=C(CN2CCNCC2)C(OC)=C1OC
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 116.67 mg/mL (438.05 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.7546 mL 18.7730 mL 37.5460 mL
5 mM 0.7509 mL 3.7546 mL 7.5092 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

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

    Solubility: ≥ 2.08 mg/mL (7.81 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

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

    Solubility: ≥ 2.08 mg/mL (7.81 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.82%

COA (247 KB) HNMR (234 KB) RP-HPLC (242 KB) LCMS (86 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.7546 mL 18.7730 mL 37.5460 mL 93.8650 mL
5 mM 0.7509 mL 3.7546 mL 7.5092 mL 18.7730 mL
10 mM 0.3755 mL 1.8773 mL 3.7546 mL 9.3865 mL
15 mM 0.2503 mL 1.2515 mL 2.5031 mL 6.2577 mL
20 mM 0.1877 mL 0.9386 mL 1.8773 mL 4.6932 mL
25 mM 0.1502 mL 0.7509 mL 1.5018 mL 3.7546 mL
30 mM 0.1252 mL 0.6258 mL 1.2515 mL 3.1288 mL
40 mM 0.0939 mL 0.4693 mL 0.9386 mL 2.3466 mL
50 mM 0.0751 mL 0.3755 mL 0.7509 mL 1.8773 mL
60 mM 0.0626 mL 0.3129 mL 0.6258 mL 1.5644 mL
80 mM 0.0469 mL 0.2347 mL 0.4693 mL 1.1733 mL
100 mM 0.0375 mL 0.1877 mL 0.3755 mL 0.9386 mL
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Trimetazidine Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Trimetazidine5011-34-7AutophagyInhibitorinhibitorinhibit

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