WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H591146
CAS#: 13171-25-0 (HCl)
Description: Trimetazidine is an inhibitor of NLRP3/GSDMD pathway-mediated pyroptosis for the treatment of dexamethasone-induced muscle atrophy. The mechanism of action of trimetazidine involves its effect on cellular energy metabolism, specifically the metabolism of fatty acids and glucose. Trimetazidine works by inhibiting a specific enzyme called long-chain 3-ketoacyl-CoA thiolase, which is involved in the beta-oxidation process of fatty acids. By blocking this enzyme, trimetazidine reduces the oxidation of fatty acids and promotes the oxidation of glucose instead. Glucose oxidation requires less oxygen consumption compared to the beta-oxidation of fatty acids.
Hodoodo Cat#: H591146
Name: Trimetazidine HCl
CAS#: 13171-25-0 (HCl)
Chemical Formula: C14H24Cl2N2O3
Exact Mass: 338.12
Molecular Weight: 339.250
Elemental Analysis: C, 49.57; H, 7.13; Cl, 20.90; N, 8.26; O, 14.15
Related CAS #: 13171-25-0 (HCl) 5011-34-7 (free base)
Synonym: Trimetazidine hydrochloride;
IUPAC/Chemical Name: Piperazine, 1-((2,3,4-trimethoxyphenyl)methyl)-, dihydrochloride (9CI)
InChi Key: VYFLPFGUVGMBEP-UHFFFAOYSA-N
InChi Code: InChI=1S/C14H22N2O3.2ClH/c1-17-12-5-4-11(13(18-2)14(12)19-3)10-16-8-6-15-7-9-16;;/h4-5,15H,6-10H2,1-3H3;2*1H
SMILES Code: COC1=CC=C(CN2CCNCC2)C(OC)=C1OC.[H]Cl.[H]Cl
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info: Trimetazidine (TMZ) is a medication used to treat cardiovascular disorders, including angina pectoris , or sudden chest, jaw, or back pain caused by reduced blood flow to the heart. It helps the body metabolize fatty acids, which helps it use oxygen, and allows for more blood flow to the heart. This can help lessen chest pain from blocked blood vessels. TMZ is sold under many brand names and is described as the first cytoprotective anti-ischemic agent developed and marketed by Laboratoires Servier. It's suitable for initial use as monotherapy in patients with angina pectoris, and as adjunctive therapy in those with symptoms not sufficiently controlled by nitrates, beta-blockers, or calcium antagonists .
| Biological target: | Trimetazidine is an inhibitor of NLRP3/GSDMD pathway-mediated pyroptosis for the treatment of dexamethasone-induced muscle atrophy. The mechanism of action of trimetazidine involves its effect on cellular energy metabolism, specifically the metabolism of fatty acids and glucose. Trimetazidine works by inhibiting a specific enzyme called long-chain 3-ketoacyl-CoA thiolase, which is involved in the beta-oxidation process of fatty acids. By blocking this enzyme, trimetazidine reduces the oxidation of fatty acids and promotes the oxidation of glucose instead. Glucose oxidation requires less oxygen consumption compared to the beta-oxidation of fatty acids. |
| In vitro activity: | Trimetazidine (TMZ) is an anti-ischemic agent that can inhibit the fatty acid oxidation. It has been stated that inhibition of fatty acid oxidation may be an acceptable approach to cancer treatment. This study examined the effects of administration on viability and other variables of human pancreatic cells, and found that TMZ can induce cytotoxicity and apoptosis and reduce migration and ATP levels. A combination strategy based on inhibition of fatty acid oxidation and anticancer drugs may be more effective in the treatment of pancreatic cancers. Clin Res Hepatol Gastroenterol. 2021 Nov;45(6):101632. https://pubmed.ncbi.nlm.nih.gov/33662778/ |
| In vivo activity: | As a metabolic modulator, trimetazidine improves glucose metabolism. Furthermore, trimetazidine enhances mitochondrial metabolism and promotes nerve regeneration, exerting an anti-inflammatory and antioxidant effect. This study treated mice with trimetazidine and fount that administration delays motor function decline, improves muscle performance and metabolism, and significantly extends overall survival of SOD1G93A mice (increased median survival of 16 days and 12.5 days for male and female respectively). Moreover, trimetazidine prevents the degeneration of neuromuscular junctions, attenuates motor neuron loss and reduces neuroinflammation in the spinal cord and in peripheral nerves. Br J Pharmacol. 2022 Apr;179(8):1732-1752. https://pubmed.ncbi.nlm.nih.gov/34783031/ |
The following data is based on the product molecular weight 339.25 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | 1. Bortolasci CC, Kidnapillai S, Spolding B, Truong TTT, Connor T, Swinton C, Panizzutti B, Liu ZSJ, Sanigorski A, Dean OM, Crowley T, Richardson M, Bozaoglu K, Vlahos K, Cowdery S, Watmuff B, Steyn SF, Wolmarans W, Engelbrecht BJ, Perry C, Drummond K, Pang T, Jamain S, Gray L, McGee SL, Harvey BH, Kim JH, Leboyer M, Berk M, Walder K. Use of a gene expression signature to identify trimetazidine for repurposing to treat bipolar depression. Bipolar Disord. 2023 Dec;25(8):661-670. doi: 10.1111/bdi.13319. Epub 2023 Mar 23. PMID: 36890661; PMCID: PMC10946906. 2. Atlı Şekeroğlu Z, Şekeroğlu V, Işık S, Aydın B. Trimetazidine alone or in combination with gemcitabine and/or abraxane decreased cell viability, migration and ATP levels and induced apoptosis of human pancreatic cells. Clin Res Hepatol Gastroenterol. 2021 Nov;45(6):101632. doi: 10.1016/j.clinre.2021.101632. Epub 2021 Mar 1. PMID: 33662778. 3. Scaricamazza S, Salvatori I, Amadio S, Nesci V, Torcinaro A, Giacovazzo G, Primiano A, Gloriani M, Candelise N, Pieroni L, Loeffler JP, Renè F, Quessada C, Tefera TW, Wang H, Steyn FJ, Ngo ST, Dobrowolny G, Lepore E, Urbani A, Musarò A, Volonté C, Ferraro E, Coccurello R, Valle C, Ferri A. Repurposing of Trimetazidine for amyotrophic lateral sclerosis: A study in SOD1G93A mice. Br J Pharmacol. 2022 Apr;179(8):1732-1752. doi: 10.1111/bph.15738. Epub 2022 Jan 13. PMID: 34783031; PMCID: PMC9305494. 4. Wang L, Jiao XF, Wu C, Li XQ, Sun HX, Shen XY, Zhang KZ, Zhao C, Liu L, Wang M, Bu YL, Li JW, Xu F, Chang CL, Lu X, Gao W. Trimetazidine attenuates dexamethasone-induced muscle atrophy via inhibiting NLRP3/GSDMD pathway-mediated pyroptosis. Cell Death Discov. 2021 Sep 18;7(1):251. doi: 10.1038/s41420-021-00648-0. PMID: 34537816; PMCID: PMC8449784. |
| In vitro protocol: | 1. Bortolasci CC, Kidnapillai S, Spolding B, Truong TTT, Connor T, Swinton C, Panizzutti B, Liu ZSJ, Sanigorski A, Dean OM, Crowley T, Richardson M, Bozaoglu K, Vlahos K, Cowdery S, Watmuff B, Steyn SF, Wolmarans W, Engelbrecht BJ, Perry C, Drummond K, Pang T, Jamain S, Gray L, McGee SL, Harvey BH, Kim JH, Leboyer M, Berk M, Walder K. Use of a gene expression signature to identify trimetazidine for repurposing to treat bipolar depression. Bipolar Disord. 2023 Dec;25(8):661-670. doi: 10.1111/bdi.13319. Epub 2023 Mar 23. PMID: 36890661; PMCID: PMC10946906. 2. Atlı Şekeroğlu Z, Şekeroğlu V, Işık S, Aydın B. Trimetazidine alone or in combination with gemcitabine and/or abraxane decreased cell viability, migration and ATP levels and induced apoptosis of human pancreatic cells. Clin Res Hepatol Gastroenterol. 2021 Nov;45(6):101632. doi: 10.1016/j.clinre.2021.101632. Epub 2021 Mar 1. PMID: 33662778. |
| In vivo protocol: | 1. Scaricamazza S, Salvatori I, Amadio S, Nesci V, Torcinaro A, Giacovazzo G, Primiano A, Gloriani M, Candelise N, Pieroni L, Loeffler JP, Renè F, Quessada C, Tefera TW, Wang H, Steyn FJ, Ngo ST, Dobrowolny G, Lepore E, Urbani A, Musarò A, Volonté C, Ferraro E, Coccurello R, Valle C, Ferri A. Repurposing of Trimetazidine for amyotrophic lateral sclerosis: A study in SOD1G93A mice. Br J Pharmacol. 2022 Apr;179(8):1732-1752. doi: 10.1111/bph.15738. Epub 2022 Jan 13. PMID: 34783031; PMCID: PMC9305494. 2. Wang L, Jiao XF, Wu C, Li XQ, Sun HX, Shen XY, Zhang KZ, Zhao C, Liu L, Wang M, Bu YL, Li JW, Xu F, Chang CL, Lu X, Gao W. Trimetazidine attenuates dexamethasone-induced muscle atrophy via inhibiting NLRP3/GSDMD pathway-mediated pyroptosis. Cell Death Discov. 2021 Sep 18;7(1):251. doi: 10.1038/s41420-021-00648-0. PMID: 34537816; PMCID: PMC8449784. |
1: Pramana KAAP, Cahyani NGAMSD, Pintaningrum Y, Rahmat B. New insight of the efficacy trimetazidine in patients with peripheral arterial disease: a meta- analysis. Egypt Heart J. 2024 Mar 6;76(1):31. doi: 10.1186/s43044-024-00461-x. PMID: 38448715; PMCID: PMC10917706.
2: Pușcaș A, Ștefănescu R, Vari CE, Ősz BE, Filip C, Bitzan JK, Buț MG, Tero- Vescan A. Biochemical Aspects That Lead to Abusive Use of Trimetazidine in Performance Athletes: A Mini-Review. Int J Mol Sci. 2024 Jan 28;25(3):1605. doi: 10.3390/ijms25031605. PMID: 38338885; PMCID: PMC10855343.
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