盐酸曲美他嗪作用机制 - Medchemexpress - MCE中国

1、Product Data SheetTrimetazidine dihydrochlorideCat. No.: HY-B0968CAS No.: 13171-25-0分式: CHClNO分量: 339.26作靶点: Autophagy作通路: Autophagy储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 H2O : 100 mg/mL (294.76 mM)DMSO : 25 mg/mL (73.69 mM; Need ultrasonic)* means soluble, b

2、ut saturation unknown.SolventMass1 mg 5 mg 10 mgConcentration制备储备液1 mM 2.9476 mL 14.7380 mL 29.4759 mL5 mM 0.5895 mL 2.9476 mL 5.8952 mL10 mM 0.2948 mL 1.4738 mL 2.9476 mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 储存时，请在 6 个内使，-20C 储存时，请在 1 个内

3、使。体内实验请根据您的实验动物和给药式选择适当的溶解案。以下溶解案都请先按照 In Vitro 式配制澄清的储备液，再依次添加助溶剂：为保证实验结果的可靠性，澄 的储备液可以根据储存条件，适当保存；体内实验的作液，建议您现现配，当天使； 以下溶剂前显的百分 指该溶剂在您配制终溶液中的体积占；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的式助溶1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (7.37 mM); Clear solution此案可获得 2.5 mg/mL (7.

4、37 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 400 L PEG300 中，混合均匀；向上述体系中加50 L Tween-80，混合均匀；然后继续加 450 L 理盐定容 1 mL。2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (7.37 mM); Clear solutionPage 1 of 2 www.MedChemE此案可获得 2.5 mg/mL (7.37 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为

5、例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 900 L 20% 的 SBE-CD 理盐溶液中，混合均匀。BIOLOGICAL ACTIVITY物活性 Trimetazidine dihydrochloride 种选择性的长链 3-ketoyl coenzyme A thiolase 抑制剂，IC50 值为 75 nM，可抑制 游离脂 酸的 -氧化。Trimetazidine dihydrochloride 种有效的抗绞痛药和种细胞保护药，具有抗氧化，抗炎 ，抗伤害和胃保护作。Trimetazidine dihydrochloride 诱导噬，还 种 HADHA 抑制剂

6、。IC & Target IC50: 75 nM (long chain 3-ketoyl coenzyme A thiolase)2-oxidation2Autophagy33-hydroxyacyl-CoA dehydrogenase (HADHA)4体外研究 Trimetazidine (1 M-100 M; 24 hours; HUVECs) could enhance the viability of the injured HUVECs induces byoxidation in a certain dose-dependent manner1.Cell Viability As

7、say1Cell Line: Human umbilical vein endothelial cells (HUVECs)Concentration: 1 M, 10 M, 100 MIncubation Time: 24 hoursResult: Enhanced the viability of the injured HUVECs induced by oxidation.体内研究 Trimetazidine (5-20 mg/kg; oral administration; 1 hour; Swiss albino male mice) in 10 mg/kg and 20 mg/k

8、g dosessignificantly raises the seizure-threshold current in the increasing current electroshock seizure (ICES) test in the mice5.Animal Model: Swiss albino male mice (24-35 g)4Dosage: 5 mg/kg, 10 mg/kg and 20 mg/kg;10 mL/kg body weightAdministration: Oral administration; 1 hourResult: In 10 mg/kg a

9、nd 20 mg/kg doses significantly raised the seizure-threshold current inthe ICES test.户使本产品发表的科研献 Anatol J Cardiol. 2019; 22: 00-00.See more customer validations on HYPERLINK www.MedChemE www.MedChemEPage 2 of 3 www.MedChemEREFERENCES1. Shenghu He, et al. Protective effects of trimetazidine against v

10、ascular endothelial cell injury induced by oxidation. Journal of Geriatric Cardiology,December 2008 , Vol 5 No 4.2. Jain S, et al. Trimetazidine exerts protection against increasing current electroshock seizure test in mice. Seizure. 2010 Jun;19(5):300-2.3. Kantor PF, et al. The antianginal drug tri

11、metazidine shifts cardiac energy metabolism from fatty acid oxidation to glucose oxidation by inhibitingmitochondrial long-chain 3-ketoacyl coenzyme A thiolase. Circ Res. 2000 Mar 17;86(5):580-8.4. Chrusciel P, et al. Defining the role of trimetazidine in the treatment of cardiovascular disorders: s

12、ome insights on its role in heart failure and peripheralartery disease. Drugs. 2014 Jun;74(9):971-80.5. Hossain F, et al.Inhibition of Fatty Acid Oxidation Modulates Immunosuppressive Functions of Myeloid-Derived Suppressor Cells and Enhances CancerTherapies. Cancer Immunol Res. 2015 Nov;3(11):1236-47.McePdfHeightCaution: Product has not been