Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ezetimibe (SCH 58235) 是一种膳食胆固醇吸收抑制剂。它是一种NPC1L1抑制剂,是有效的Nrf2激活剂。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
10 mg | ¥ 287 | 现货 | ||
25 mg | ¥ 463 | 现货 | ||
50 mg | ¥ 592 | 现货 | ||
100 mg | ¥ 828 | 现货 | ||
200 mg | ¥ 1,220 | 现货 | ||
500 mg | ¥ 1,980 | 现货 | ||
1 g | ¥ 2,970 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 413 | 现货 |
产品描述 | Ezetimibe (SCH 58235) is a Dietary Cholesterol Absorption Inhibitor. The physiologic effect of ezetimibe is by means of Decreased Cholesterol Absorption. |
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。 |
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]. |
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]. |
别名 | 依泽替米贝, SCH 58235 |
分子量 | 409.43 |
分子式 | C24H21F2NO3 |
CAS No. | 163222-33-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 75 mg/mL (183.2 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: 75 mg/mL (183.2 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 2.4424 mL | 12.2121 mL | 24.4242 mL | 61.0605 mL |
5 mM | 0.4885 mL | 2.4424 mL | 4.8848 mL | 12.2121 mL | |
10 mM | 0.2442 mL | 1.2212 mL | 2.4424 mL | 6.106 mL | |
20 mM | 0.1221 mL | 0.6106 mL | 1.2212 mL | 3.053 mL | |
50 mM | 0.0488 mL | 0.2442 mL | 0.4885 mL | 1.2212 mL | |
100 mM | 0.0244 mL | 0.1221 mL | 0.2442 mL | 0.6106 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Ezetimibe 163222-33-1 Autophagy Immunology/Inflammation Membrane transporter/Ion channel Others Nrf2 NPC1L1 SCH58235 依泽替米贝 inhibit Keap1-Nrf2 Inhibitor SCH 58235 SCH-58235 inhibitor