D0302 | Trimetazidine
C
C01EB15 Trimetazidine
[C01EB] Other cardiac preparations
[C01E] OTHER CARDIAC PREPARATIONS
[C01] CARDIAC THERAPY
[C] Cardiovascular system
| Toxicity | Dose | Time | Species | Model | Method | Action | Positive criterion | Reference |
|---|---|---|---|---|---|---|---|---|
| GLYCOLYSIS | increase | 17 | ||||||
| FATTY ACID METABOLISM | 100 μM | 24hr | T47D cells | quantifies the conversion of [9,10-3H(N)]-palmitic acid to 3H2O with diffusion | stimulate | Student’s two-tail t-test, where p < 0.05 | 273 | |
| MITOCHONDRIAL FATTY ACID BETA OXIDATION | decrease | 17 | ||||||
| MITOCHONDRIAL FATTY ACID BETA OXIDATION | 20.5/>100 | human/rat | hepatocytes | Fatty acid oxidation (FAO) was determined by measuring 14CO2 release from 14C-labeled palmitate | inhibition | IC50 (μM) | 333 | |
| SYNTHESIS OF KETONE BODY | 47.1 | Wistar rat | hepatocytes | ketone bodies (KB = β-hydroxybutyrate + acetoacetate) were determined with a commercially available kit (Autokit 3-HB from Wako) | inhibition | IC50 (μM) | 333 | |
| TRANSPORT OF CALCIUM | 10-100µM | rat | isolated cardiac mitochondria | increase | 274 | |||
| Target | Dose | Time | Species | Model | Method | Action | Positive criterion | Reference |
|---|---|---|---|---|---|---|---|---|
| Carnitine O-palmitoyltransferase 1, liver isoform, CPT1-L, EC 2.3.1.21 | >100/− | human/rat | recombinant Pichia pastoris Membrane Preparations | spectrophotometric assay with DTNB | Negative | IC50 (μM) | 333 | |
| Carnitine O-palmitoyltransferase 1, muscle isoform | >100 | human/rat | recombinant Pichia pastoris Membrane Preparations | spectrophotometric assay with DTNB | Negative | IC50 (μM) | 333 | |
| Carnitine O-palmitoyltransferase 2, mitochondrial, EC 2.3.1.21 | >100/− | human/rat | recombinant Pichia pastoris Membrane Preparations | spectrophotometric assay with DTNB | Negative | IC50 (μM) | 333 | |
| Pictogram | Signal | Statements | Precautionary Statement Codes |
|---|---|---|---|
   |
Danger |
Aggregated GHS information provided by 3 companies from 2 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies. H226 (66.67%): Flammable liquid and vapor [Warning Flammable liquids] H302 (66.67%): Harmful if swallowed [Warning Acute toxicity, oral] H314 (66.67%): Causes severe skin burns and eye damage [Danger Skin corrosion/irritation] H315 (33.33%): Causes skin irritation [Warning Skin corrosion/irritation] H319 (33.33%): Causes serious eye irritation [Warning Serious eye damage/eye irritation] H335 (33.33%): May cause respiratory irritation [Warning Specific target organ toxicity, single exposure Respiratory tract irritation] H412 (66.67%): Harmful to aquatic life with long lasting effects [Hazardous to the aquatic environment, long-term hazard] Information may vary between notifications depending on impurities, additives, and other factors. The percentage value in parenthesis indicates the notified classification ratio from companies that provide hazard codes. Only hazard codes with percentage values above 10% are shown. |
P210, P233, P240, P241, P242, P243, P260, P261, P264, P270, P271, P273, P280, P301+P312, P301+P330+P331, P302+P352, P303+P361+P353, P304+P340, P305+P351+P338, P310, P312, P321, P330, P332+P313, P337+P313, P362, P363, P370+P378, P403+P233, P403+P235, P405, and P501; (The corresponding statement to each P-code can be found at the GHS Classification page.) |
| Organism | Test type | Route | Dose (normalized dose) | Effect | Source |
|---|---|---|---|---|---|
| rat | LD50 | intraperitoneal | 345mg/kg (345mg/kg) | Drugs in Japan Vol. 6, Pg. 527, 1982. | |
| mouse | LD50 | oral | 1550mg/kg (1550mg/kg) | Drugs in Japan Vol. 6, Pg. 527, 1982. | |
| rat | LD50 | oral | 1700mg/kg (1700mg/kg) | Drugs in Japan Vol. 6, Pg. 527, 1982. | |
| mouse | LD50 | intravenous | 125mg/kg (125mg/kg) | United States Patent Document. Vol. #3262852, | |
| mouse | LD50 | subcutaneous | 410mg/kg (410mg/kg) | Drugs in Japan Vol. 6, Pg. 527, 1982. | |
| rat | LD50 | subcutaneous | 1500mg/kg (1500mg/kg) | Drugs in Japan Vol. 6, Pg. 527, 1982. | |
| mouse | LD50 | intraperitoneal | 305mg/kg (305mg/kg) | United States Patent Document. Vol. #3262852, | |
| 1,2,3-trimethoxy-4-(piperazinylmethyl)benzene | 1-((2,3,4-trimethoxyphenyl)methyl)-piperazindihydrochloride;1-(2,3,4-trimethoxybenzyl)-piperazindihydrochloride | 1-(2,3,4-Trimethoxy-benzyl)-piperazine |
| 1-(2,3,4-Trimethoxybenzyl)piperazine | 1-(2,3,4-trimethoxy benzyl)piperazine | 1-(2,3,4-trimethoxybenzyl)piperazine;hydrochloride |
| 1-(2,3,4-trimethoxyphenyl)methylpiperazine | 1-(2,3,4-trimethoxyphenylmethyl)piperazine | 1-[(2,3,4-trimethoxyphenyl)methyl]piperazine |
| 1-[(2,3,4-trimethoxyphenyl)methyl]piperazine;hydrochloride | 1-[2,3,4-trimethoxybenzyl] piperazine dihydrochloride | 4-(2,3,4-Trimethoxybenzyl)piperazine |
| 5011-34-7 | 71T250 | A25088 |
| A827982 | A837947 | AB0111344 |
| AKOS000308094 | ALBB-004703 | BAS 06612844 |
| BB 0220635 | BBL013084 | BCP16534 |
| BDBM80613 | BPBio1_000657 | BRD-K88366685-300-03-7 |
| BRD-K88366685-300-04-5 | BSPBio_000597 | CAS-13171-25-0 |
| CHEBI:94789 | CHEMBL203266 | CTK4J2174 |
| D08642 | DB-051731 | DB09069 |
| DTXSID2048531 | Dilatan (TN) | EINECS 225-690-2 |
| EN300-14439 | FT-0603666 | HMS2230L07 |
| HMS3374D04 | LS-175136 | MCULE-9820869946 |
| MLS001240268 | MLS001331735 | N9A0A0R9S8 |
| NCGC00016697-01 | NCGC00016697-02 | Oprea1_279550 |
| Piperazine, 1-((2,3,4-trimethoxyphenyl)methyl)- | Piperazine, 1-[(2,3,4-trimethoxyphenyl)methyl]- | Piperazine,1-[(2,3,4-trimethoxyphenyl)methyl]- |
| Preductal | Preductal MB | Prestwick0_000549 |
| Prestwick1_000549 | Prestwick2_000549 | Prestwick3_000549 |
| Q674703 | R3927 | SBB007020 |
| SCHEMBL230374 | SMR000674573 | SMR000814701 |
| SPBio_002518 | ST45134749 | STK315643 |
| TR-004340 | TRIMETAZIDINE | Trimetazidina |
| Trimetazidina [INN-Spanish] | Trimetazidine (INN) | Trimetazidine HCl |
| Trimetazidine [INN:BAN:DCF] | Trimetazidinum | Trimetazidinum [INN-Latin] |
| UHWVSEOVJBQKBE-UHFFFAOYSA-N | UNII-N9A0A0R9S8 | Vasartel |
| Vasorel | Z99601262 | ZINC19358638 |
| cid_9926449 |
| DrugBank Name | Trimetazidine |
| DrugBank | DB09069 |
| CAS Number | 127881-54-3, 13171-25-0, 5011-34-7, 738-70-5 |
| PubChem Compound | 21109 |
| KEGG Drug | D08642 |
| PubChem.Substance | 310265002 |
| ChEBI | 94789 |
| ChemSpider | 19853 |
| BindingDB | 80613.0 |
| Wikipedia | Trimetazidine |