鹽酸曲美他嗪作用機(jī)制 - Medchemexpress - MCE中國(guó)

1、Product Data SheetTrimetazidine dihydrochlorideCat. No.: HY-B0968CAS No.: 13171-25-0分式: CHClNO分量: 339.26作靶點(diǎn): Autophagy作通路: Autophagy儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) 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制備儲(chǔ)備液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請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?6 個(gè)內(nèi)使，-20C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?1 個(gè)內(nèi)

3、使。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍?。以下溶解案都?qǐng)先按照 In Vitro 式配制澄清的儲(chǔ)備液，再依次添加助溶劑：為保證實(shí)驗(yàn)結(jié)果的可靠性，澄 的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使； 以下溶劑前顯的百分 指該溶劑在您配制終溶液中的體積占；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的式助溶1. 請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (7.37 mM); Clear solution此案可獲得 2.5 mg/mL (7.

4、37 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲(chǔ)備液加到 400 L PEG300 中，混合均勻；向上述體系中加50 L Tween-80，混合均勻；然后繼續(xù)加 450 L 理鹽定容 1 mL。2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (7.37 mM); Clear solutionPage 1 of 2 www.MedChemE此案可獲得 2.5 mg/mL (7.37 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為

5、例，取 100 L 25.0 mg/mL 的澄 DMSO 儲(chǔ)備液加到 900 L 20% 的 SBE-CD 理鹽溶液中，混合均勻。BIOLOGICAL ACTIVITY物活性 Trimetazidine dihydrochloride 種選擇性的長(zhǎng)鏈 3-ketoyl coenzyme A thiolase 抑制劑，IC50 值為 75 nM，可抑制 游離脂 酸的 -氧化。Trimetazidine dihydrochloride 種有效的抗絞痛藥和種細(xì)胞保護(hù)藥，具有抗氧化，抗炎 ，抗傷害和胃保護(hù)作。Trimetazidine dihydrochloride 誘導(dǎo)噬，還 種 HADHA 抑制劑

6、。IC & Target IC50: 75 nM (long chain 3-ketoyl coenzyme A thiolase)2-oxidation2Autophagy33-hydroxyacyl-CoA dehydrogenase (HADHA)4體外研究 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.體內(nèi)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.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) 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