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.
| Molecular Weight | 266.34 |
| CAS Number | 5011-34-7 |
| Solubility (25°C) | DMSO 90 mg/mL |
| Storage | 2-8°C, protect from light, sealed |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[2] Dvid Pintr, et al. eNeuro. Trimetazidine Use in Parkinson's Disease: Is It a Resolved Problem?
[3] Mario Marzilli, et al. Int J Cardiol. Trimetazidine in cardiovascular medicine
[4] Agustn Ciapponi, et al. Cochrane Database Syst Rev. WITHDRAWN: Trimetazidine for stable angina
[5] I V Zhirov, et al. Kardiologiia. [Trimetazidine in the Treatment of Chronic HeartFailure]
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