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Trimetazidine dihydrochloride FAO inhibitor

Name: Trimetazidine dihydrochloride
Brand: Selleck Chemicals
SKU: S4543
Availability: InStock
Rating: 5 (9 reviews)

Cat.No.S4543

Trimetazidine dihydrochloride (Yoshimilon, Kyurinett, Vastarel F) is a kind of drug for treatment of chronic ischemic disorders. It improves myocardial glucose utilization through inhibition of fatty acid metabolism, known as fatty acid oxidation inhibitor.

Chemical Structure

Molecular Weight: 339.26

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Quality Control

Batch: Purity: 99.97%

99.97

Related Targets	Dehydrogenase HSP Transferase P450 (e.g. CYP17) PDE phosphatase PPAR Vitamin Carbohydrate Metabolism Mitochondrial Metabolism
Featured Inhibitors	Y-27632 Dihydrochloride SB431542 CHIR-99021 (Laduviglusib) RMC-7977 RMC-6236 (Daraxonrasib) MRTX1133 MG132 Z-VAD-FMK VT3989 IAG933

Solubility

In vitro
Batch:

DMSO : 68 mg/mL (200.43 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 68 mg/mL

Ethanol : 5 mg/mL

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	saline Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	50.000mg/ml (147.38mM)	Taking the 1 mL working solution as an example, add 50 mg of this product to 1 ml of physiological saline (0.9% NaCL solution), mix evenly to make it clear, The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

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.

Chemical Information, Storage & Stability

Molecular Weight	339.26	Formula	C₁₄H₂₂N₂O₃.2HCl	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	13171-25-0	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	Yoshimilon, Kyurinett, Vastarel F			SMILES	COC1=C(C(=C(C=C1)CN2CCNCC2)OC)OC.Cl.Cl

Read more about storage stability stock solution CAS number SMILES

Mechanism of Action

Targets/IC₅₀/Ki	mitochondrial long-chain 3-ketoacyl thiolase (Cell-free assay) 75 nM
In vitro	Trimetazidine up-regulates miR-21 expression, then miR-21 targets PTEN increasing the PI3K pathway and finally the activation of this pathway counteracts the apoptotic effect of hypoxia/reperfusion.
In vivo	The administration of TMZ reduces myocardial infarction size in WT C57BL/6J hearts. Both AMPK and ERK signaling pathways mediate the cardioprotection of TMZ against ischemic injury. Trimetazidine Shifts Metabolism from Fatty Acid Oxidation to Glucose Oxidation and improves Contractile Functions of Cardiomyocytes during Hypoxia.
References	[1] https://pubmed.ncbi.nlm.nih.gov/10720420/ [2] https://pubmed.ncbi.nlm.nih.gov/26892523/ [3] https://pubmed.ncbi.nlm.nih.gov/26097555/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-08-31)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT07794475	RECRUITING	Diabetic Peripheral Neuropathic Pain (DPN)	Sara Refaat Azab Metry	2026-08-01	PHASE1; PHASE2
NCT05540184	UNKNOWN	AKI - Acute Kidney Injury	Beni-Suef University	2022-09-19	PHASE4
NCT06656442	COMPLETED	Acute Ischemic Stroke	Ain Shams University	2024-09-01	PHASE3
NCT06459193	COMPLETED	Peripheral Neuropathy Due to Chemotherapy	Minia University	2024-06-23	PHASE1; PHASE2
NCT06140953	COMPLETED	Metabolic Associated Fatty Liver Disease	October 6 University	2023-12-10	PHASE2
NCT05147194	UNKNOWN	Diabetic Nephropathies	Tongji Hospital	2022-01-01	PHASE2

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