| 名稱 | Ezetimibe |
| 描述 | Ezetimibe (SCH 58235) is a Dietary Cholesterol Absorption Inhibitor. The physiologic effect of ezetimibe is by means of Decreased Cholesterol Absorption. |
| 細胞實驗 | 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]. |
| 激酶實驗 | 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]. |
| 體外活性 | 有效地抑制膽固醇穿過腸壁的轉(zhuǎn)運,從而降低高膽固醇血癥的臨床前動物模型中的血漿膽固醇.Ezetimibe消除大鼠腸道的胰腺外分泌功能,同時保持膽汁流量.Ezetimibe降低膽固醇喂養(yǎng)的倉鼠的血漿膽固醇和肝膽固醇積累,ED（50）為0.04 mg/kg.Ezetimibe減少主動脈粥樣硬化病變的表面積,從對照組的20.2％到西方飲食組的4.1％和低脂肪膽固醇飲食小鼠的7.0％.Ezetimibe減少頸動脈粥樣硬化病變的橫截面面積,在西方低脂膽固醇飲食組中為97%,在無膽固醇的小鼠中為91%. |
| 體內(nèi)活性 | Ezetimibe顯著降低表面受體SR-BI,Niemann-Pick C1型類似蛋白1,ATP結(jié)合盒轉(zhuǎn)運子,亞族A和核受體維甲酸受體的γ,固醇調(diào)節(jié)元件結(jié)合蛋白-1和-2,肝X受體的β亞基的mRNA的表達。Ezetimibe明顯降低總膽固醇,LDL膽固醇和甘油三酸酯,適度增加高密度脂蛋白膽固醇。 Ezetimibe在Caco-2細胞中,將膽固醇轉(zhuǎn)運減少了31％,但不影響黃醇轉(zhuǎn)運。 |
| 存儲條件 | 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 recommended.
Ethanol : 75 mg/mL (183.18 mM), Sonication is recommended.
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| 關(guān)鍵字 | Sterol O-acyltransferase | SCH-58235 | SCH58235 | Nrf2 | NPC1L1 | Keap1-Nrf2 | Inhibitor | inhibit | Ezetimibe | Autophagy |
| 相關(guān)產(chǎn)品 | Guanidine hydrochloride | Naringin | Aceglutamide | Alginic acid | Hemin | Hydroxychloroquine | Sildenafil citrate | Stavudine | Tamoxifen | Adenosine | Paeonol | Sodium 4-phenylbutyrate |
| 相關(guān)庫 | 經(jīng)典已知活性庫 | 抗癌上市藥物庫 | 已知活性化合物庫 | 臨床失敗化合物庫 | EMA 上市藥物庫 | 抗衰老化合物庫 | FDA 上市藥物庫 | 膜蛋白靶向化合物庫 | 免疫/炎癥分子化合物庫 | 藥物功能重定位化合物庫 | 抗癌臨床化合物庫 | 抗癌藥物庫 |