| 名称 | Ezetimibe |
| 描述 | Ezetimibe (SCH 58235) is a Dietary Cholesterol Absorption Inhibitor. The physiologic effect of ezetimibe is by means of Decreased Cholesterol Absorption. |
| 细胞实验 | Ezetimibe is dissolved in DMSO and stored, and then diluted with appropriate medium before use[2]. Huh7 human hepatocytes are cultured in high glucose DMEM containing 10% FBS, 100 units/mL penicillin and 100 μg/mL streptomycin at 37°C in a 95% air/5% CO2 atmosphere. Hepatocytes are treated with or without Ezetimibe (10 μM, 1 h) and incubated with palmitic acid (PA, 0.5 mM, 24 h)[2]. |
| 激酶实验 | GST-p62 is prepared from Escherichia coli and 0.5 μg of the purified GST-p62 protein is used for in vitro AMPK phosphorylation assay. Phosphorylation of p62 protein by AMPK is determined by non-radioisotope method using γS-ATP. AMPK complex is immuno-purified from the HEK293 cells, to which either myc-AMPKα1 wild-type (WT) or myc-AMPKα1 kinase-dead mutant (KD, D157A) is transfected with Flag-AMPKβ1 and HA-AMPKγ1. AMPK complex is added into the reaction mixture containing 20 mM HEPES, pH7.4, 1 mM EGTA, 0.4 mM EDTA, 5 mM MgCl2, 0.05 mM DTT, 0.5 μg GST-p62, 0.2 mM AMP, and 1 mM ATPγS. Reaction is carried out at 37°C for 30 min, and then terminated by adding 20 mM EDTA. To detect γS-labeled p62 protein, the reaction product is alkylated with 2.5 mM PNBM for 2 h at room temperature and analyzed the products by western blotting using anti-thiophosphate antibody[1]. |
| 体外活性 | 有效地抑制胆固醇穿过肠壁的转运,从而降低高胆固醇血症的临床前动物模型中的血浆胆固醇.Ezetimibe消除大鼠肠道的胰腺外分泌功能,同时保持胆汁流量.Ezetimibe降低胆固醇喂养的仓鼠的血浆胆固醇和肝胆固醇积累,ED（50）为0.04 mg/kg.Ezetimibe减少主动脉粥样硬化病变的表面积,从对照组的20.2％到西方饮食组的4.1％和低脂肪胆固醇饮食小鼠的7.0％.Ezetimibe减少颈动脉粥样硬化病变的横截面面积,在西方低脂胆固醇饮食组中为97%,在无胆固醇的小鼠中为91%. |
| 体内活性 | Ezetimibe显著降低表面受体SR-BI,Niemann-Pick C1型类似蛋白1,ATP结合盒转运子,亚族A和核受体维甲酸受体的γ,固醇调节元件结合蛋白-1和-2,肝X受体的β亚基的mRNA的表达。Ezetimibe明显降低总胆固醇,LDL胆固醇和甘油三酸酯,适度增加高密度脂蛋白胆固醇。 Ezetimibe在Caco-2细胞中,将胆固醇转运减少了31％,但不影响黄醇转运。 |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | DMSO : 260 mg/mL (635.03 mM), Sonication is recommended.
H2O : < 1 mg/mL (insoluble or slightly soluble)
10% DMSO+90% Corn Oil : 2.5 mg/mL (6.11 mM), Sonication is recommeded.
Ethanol : 75 mg/mL (183.18 mM), Sonication is recommended.
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| 关键字 | Sterol O-acyltransferase | SCH-58235 | SCH58235 | Nrf2 | NPC1L1 | Keap1-Nrf2 | Inhibitor | inhibit | Ezetimibe | Autophagy |
| 相关产品 | Naringin | Guanidine hydrochloride | L-Methionine | Aceglutamide | Alginic acid | Cysteamine hydrochloride | Hemin | Hydroxychloroquine | Stavudine | Tamoxifen | Paeonol | Sodium 4-phenylbutyrate |
| 相关库 | 抑制剂库 | 抗癌上市药物库 | 经典已知活性库 | 已知活性化合物库 | 临床失败化合物库 | EMA 上市药物库 | FDA 上市药物库 | 膜蛋白靶向化合物库 | 神经退行性疾病化合物库 | 药物功能重定位化合物库 | 抗癌临床化合物库 | 抗癌药物库 |