[CAS NO. 13171-25-0]??Trimetazidine dihydrochloride
PRODUCTS SPECIFICATIONS [13171-25-0]
DESCRIPTION [13171-25-0]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 339.26 |
| Molecular Formula | C14H24Cl2N2O3 |
| SMILES | COC1=CC=C(CN2CCNCC2)C(OC)=C1OC.[H]Cl.[H]Cl |
4 Publications Citing Use of MCE
Summary
Trimetazidine dihydrochloride is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC 50 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
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
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT04702906 | Tanta University |
Aluminum Phosphide Poisoning
|
February 2021 | Not Applicable |
| NCT04511520 | National Research Center for Preventive Medicine|National Medical Research Center for Therapy and Preventive Medicine |
Atrial Fibrillation Paroxysmal
|
July 2013 | Not Applicable |
| NCT03333499 | Dalian University |
Chronic Heart Failure
|
November 1, 2017 | Phase 1 |
| NCT03809273 | Shenyang Northern Hospital |
Percutaneous Coronary Intervention
|
August 1, 2019 | Phase 4 |
| NCT04760821 | Ministry of Health, Brazil|InCor Heart Institute |
Acute Respiratory Distress Syndrome|Covid19|Myocardial Injury
|
December 10, 2020 | Phase 2 |
| NCT03278444 | The First Affiliated Hospital of Zhengzhou University|First Affiliated Hospital of Xinjiang Medical University|Jiaozuo third people′s hospital|Luoyang Central Hospital|Nanyang Central Hospital|Anyang Tumor Hospital|Pingmei Shenma Medical Group General Hospital|First People′s Hospital of Shangqiu |
HCC
|
July 18, 2017 | Phase 3 |
| NCT03072121 | Jun Li|Shanghai Hutchison Pharmaceuticals Limited|Guang′anmen Hospital of China Academy of Chinese Medical Sciences |
Coronary Artery Disease(CAD)
|
June 2017 | Phase 4 |
| NCT01857921 | Yonsei University |
Coronary Artery
|
December 2010 | Not Applicable |
| NCT03887013 | China National Center for Cardiovascular Diseases |
Coronary Heart Disease|Diastolic Dysfunction
|
March 25, 2019 | Phase 4 |
| NCT03737448 | Martin Pharmaceuticals |
Acute-On-Chronic Liver Failure
|
November 28, 2018 | Phase 1 |
| NCT02102672 | Pontificia Universidad Catolica de Chile|Fondo Nacional de Desarrollo Científico y Tecnológico, Chile |
Pulmonary Artery Hypertension
|
March 2014 | Phase 2 |
| NCT01696370 | University College, London|British Heart Foundation |
Hypertrophic Cardiomyopathy
|
April 2012 | Phase 2 |
| NCT04788745 | The University of Queensland|FightMND|UMC Utrecht|King′s College London|Julius Clinical |
Amyotrophic Lateral Sclerosis|Motor Neuron Disease
|
June 29, 2021 | Phase 2 |
| NCT03603249 | The University of The West Indies |
Platelet Dysfunction Due to Drugs
|
July 1, 2018 | Phase 2 |
| NCT04661709 | Guang′anmen Hospital of China Academy of Chinese Medical Sciences|Special Project of National Traditional Chinese Medicine Clinical Research Base of State Administration of Traditional Chinese Medicine|National Natural Science Foundation of China |
Coronary Heart Disease|Unstable Angina|Chinese Herbal Medicine
|
March 1, 2021 | Phase 4 |
| NCT03273387 | Indonesia University |
Precapillary Pulmonary Hypertension
|
September 10, 2017 | Phase 2|Phase 3 |
| NCT03504202 | Shanghai 10th People′s Hospital |
Patients With INOCA(Ischemia and no Obstructive Coronary Artery Disease) Who Have Coronary Microvascular Dysfunction
|
March 1, 2019 | Not Applicable |
| NCT05147194 | Tongji Hospital |
Diabetic Nephropathies
|
January 1, 2022 | Phase 2 |
| NCT00282360 | IRCCS San Raffaele |
Coronary Artery Disease|Type II Diabetes Mellitus
|
February 1999 | Phase 4 |
| NCT03715582 | University of Sao Paulo General Hospital |
Diabetes Mellitus|Angina, Unstable
|
October 1, 2018 | Phase 3 |
| NCT04939857 | Peking University Third Hospital |
Cardiotoxicity
|
June 25, 2021 | Phase 2|Phase 3 |
| NCT02107144 | Clinical Hospital Center Zemun |
Coronary Artery Disease|Microcirculation|Vascular Resistance
|
April 2014 | Phase 4 |
| NCT02826616 | Chinese PLA General Hospital |
Cardiovascular Diseases
|
July 2016 | Not Applicable |
| NCT05540184 | Beni-Suef University|Cairo University |
AKI - Acute Kidney Injury
|
September 2022 | Phase 4 |
| NCT05556005 | Ain Shams University |
Diabetes Mellitus, Type 2|Diabetic Cardiomyopathies
|
September 18, 2022 | Phase 2 |
| NCT03072082 | Jun Li|China Academy of Chinese Medical Sciences|Guang′anmen Hospital of China Academy of Chinese Medical Sciences |
Coronary Artery Disease(CAD)
|
June 2017 | Phase 4 |
| NCT03274427 | The First Affiliated Hospital of Zhengzhou University|First Affiliated Hospital of Xinjiang Medical University|Luoyang Central Hospital|Nanyang Central Hospital|Anyang Tumor Hospital|Shenma Medical Group General Hospital|First People′s Hospital of Shangqiu|Jiaozuo third people′s hospital |
HCC
|
July 18, 2017 | Phase 3 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
H 2 O : ≥ 100 mg/mL ( 294.76 mM )
DMSO : 25 mg/mL ( 73.69 mM ; Need ultrasonic)
* "≥" means soluble, but saturation unknown.
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 |
-
1.
Add each solvent one by one: PBS
Solubility: 100 mg/mL (294.76 mM); Clear solution; Need ultrasonic
-
2.
-
3.
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
References
- [1] Shenghu He, et al. Protective effects of trimetazidine against vascular endothelial cell injury induced by oxidation. Journal of Geriatric Cardiology, December 2008 , Vol 5 No 4.
- [2] Chrusciel P, et al. Defining the role of trimetazidine in the treatment of cardiovascular disorders: some insights on its role in heart failure and peripheral artery disease. Drugs. 2014 Jun;74(9):971-80.
- [3] Kantor PF, et al. The antianginal drug trimetazidine shifts cardiac energy metabolism from fatty acid oxidation to glucose oxidation by inhibiting mitochondrial long-chain 3-ketoacyl coenzyme A thiolase. Circ Res. 2000 Mar 17;86(5):580-8.
- [4] Hossain F, et al.Inhibition of Fatty Acid Oxidation Modulates Immunosuppressive Functions of Myeloid-Derived Suppressor Cells and Enhances Cancer Therapies. Cancer Immunol Res. 2015 Nov;3(11):1236-47.
- [5] Jain S, et al. Trimetazidine exerts protection against increasing current electroshock seizure test in mice. Seizure. 2010 Jun;19(5):300-2.
Synonyms