Trimetazidine 是一种选择性的长链 3-酮酰辅酶 A 硫解酶抑制剂 |MedChemExpress (MCE)

中文名：曲美他嗪

CAS：5011-34-7

品牌：MedChemExpress (MCE)

存储条件：4°C, protect from light, stored under nitrogen

生物活性：Trimetazidine 是一种选择性的长链 3-酮酰辅酶 A 硫解酶抑制剂，IC50 为 75 nM，可抑制 β-游离脂肪酸 (FFA) 的氧化。 Trimetazidine 是一种有效的抗心绞痛药和细胞保护药，具有抗氧化、抗炎、镇痛和胃保护作用。曲美他嗪触发自噬。曲美他嗪还是一种3-羟酰基辅酶 A 脱氢酶 (HADHA) 抑制剂[1][2][3][4]。 IC50 和目标：IC50：75 nM（长链 3-酮酰辅酶 A 硫解酶）[2]
β-氧化[2]自噬[3]3-羟基酰基辅酶 A 脱氢酶 (HADHA)[4]  

体外：Trimetazidine (1-100 μM; 24 hours; HUVECs) 以一定的剂量依赖方式增强氧化诱导损伤的 HUVECs 的活力[1]。

体内：曲美他嗪（5-20 mg/kg；口服给药；1 小时；瑞士白化雄性小鼠）在 10 和 20 mg/kg 剂量下显着提高小鼠 ICES 试验中的癫痫发作阈值电流[5]。

参考详情：Trimetazidine (曲美他嗪) - 仅供科研 | Antianginal Agent | MCE

 

参考文献：

[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]. 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.

[3]. Jain S, et al. Trimetazidine exerts protection against increasing current electroshock seizure test in mice. Seizure. 2010 Jun;19(5):300-2.

[4]. 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.

[5]. 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.