辛伐他汀 T0687

Product Introduction
Bioactivity


英文名: Simvastatin

描述: Simvastatin (MK 733) 是一种 HMG-CoA 还原酶抑制剂 (Ki=0.2 nM)，具有口服活性。Simvastatin 具有降血脂活性，可以抑制肝脏产生胆固醇，还可以用于预防心血管疾病。

激酶实验: For assessment of Akt protein kinase activity in vitro, substrate (2 μg histone H2B or 25 μg eNOS peptide) is incubated with Akt immunoprecipitated from cell lysate using goat polyclonal anti-Akt1 antibody. Kinase reactions are initiated following the addition of reaction components to a final concentration of ATP (50 μM) containing 10 μCi of 32P-γATP, dithiotreitol (1 mM), HEPES buffer (20 mM, pH 7.4), MnCl2 (10 mM), MgCl2 (10 mM). After incubation for 30 min at 30°C, phosphorylated histone H2B is visualized after SDS-PAGE (15%) and autoradiography. To estimate the extent of 32P incorporation into eNOS peptides, each reaction mixture is measured by spotting onto phosphocellulose disc filter and the amount of phosphate incorporated is measured by Cerenkov counting. The wild-type peptide sequence is 1174-RIRTQSFSLQERHLRGAVPWA-1194, and the mutant eNOS peptide is identical except that serine 1179 is substituted by alanine.

体外活性: 方法：BCa 细胞 5637、EJ 和 T24 用含 Simvastatin (0.5-40 µM) 处理 48 h，使用 MTT assay 检测细胞活力。结果：Simvastatin 以剂量依赖的方式显著抑制了三种 BCa 细胞的存活 。[1]方法：人成纤维细胞 SAEC 和四种肿瘤细胞 MCF7、HepG2、NCH、NCI 用 Simvastatin (20 µM) 处理 72 h，使用 TUNEL 检测细胞凋亡情况。结果：Simvastatin 可诱导不同类型的人肿瘤细胞发生凋亡，但不诱导 SAEC 细胞发生明显的凋亡。[2]

体内活性: 方法：为研究体内活性，将 Simvastatin (60 mg/kg，aqueous 2% DMSO+30% PEG 400+5% Tween 80) 灌胃给药给 C57BL/6J 小鼠，每天一次，持续六周，给予 CF 饮食。结果：Simvastatin 治疗使血清胆固醇水平降低了 18%，视网膜胆固醇和脂蛋白胆固醇含量分别降低了 24% 和 21%。[3]方法：为检测体内抗肿瘤活性，将 Simvastatin (5-50 mg/kg in methylcellulose) 灌胃给药 BALB/c nu/nu 小鼠，每天一次，持续三天。随后将结直肠癌细胞 COLO205 皮下接种到小鼠右侧。结果：Simvastatin 通过诱导肿瘤细胞凋亡和抑制肿瘤血管生成抑制异种移植小鼠模型中的肿瘤生长。[4]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: Ethanol : 31.4 mg/mL (75 mM)
DMSO : 50 mg/mL (119.45 mM)


关键字: HMG-CoA Reductase (HMGCR) | Huh7 | HepG2 | anticancer | Mitophagy | Autophagy | Simvastatin | MK733 | MK-733 | Inhibitor | Ferroptosis | inhibit | oral activity | Apoptosis | MK0733 | MK 0733 | anti-proliferation activity | cholesterol synthesis | Mitochondrial Autophagy

相关产品: SKI V | Trolox | A-1210477 | YK-4-279 | Scoulerine | RHPS4 | Sulforaphene | ranaconitine | ACBI1 | Kaempferol

相关库: Anti-Neurodegenerative Disease Compound Library | Drug Repurposing Compound Library | Anti-Cancer Drug Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | Anti-Cancer Approved Drug Library | EMA Approved Drug Library | Autophagy Compound Library | Cuproptosis Compound Library | Microbial Natural Product Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途