Trimetazidine

CAS: 5011-34-7 F: C14H22N2O3 W: 266.34

Trimetazidine is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC50 of 75 nM, which can inhibit

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Bioactivity	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 drug, 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].
Target	IC50: 75 nM (long chain 3-ketoyl coenzyme A thiolase)β-oxidationAutophagy3-hydroxyacyl-CoA dehydrogenase (HADHA)
Invitro	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]. Cell Viability Assay[1] Cell Line:
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]. Animal Model:
Name	Trimetazidine
CAS	5011-34-7
Formula	C14H22N2O3
Molar Mass	266.34
Appearance	Oil
Transport	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)
Reference	[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.