Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Selisistat (EX-527) 是一种有效且特异性的 SIRT1 抑制剂,IC50值为 38 nM,可用于研究多种亨廷顿病动物和细胞模型的病理学。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 179 | 现货 | ||
5 mg | ¥ 397 | 现货 | ||
10 mg | ¥ 528 | 现货 | ||
25 mg | ¥ 913 | 现货 | ||
50 mg | ¥ 1,330 | 现货 | ||
100 mg | ¥ 1,730 | 现货 | ||
200 mg | ¥ 2,460 | 现货 | ||
500 mg | ¥ 3,550 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 437 | 现货 |
产品描述 | Selisistat (EX-527) is an effective and specific SIRT1 inhibitor (IC50: 38 nM) and shows >200-fold selectivity against SIRT2/3. |
靶点活性 | SIRT1:38 nM(cell free) |
体外活性 | Treatment with Selisistat (EX-527) dramatically increased acetylation at lysine 382 of p53 after different types of DNA damage in primary human mammary epithelial cells and several cell lines. Inhibition of SIRT1 catalytic activity by EX-527 had no effect on cell growth, viability, or p53-controlled gene expression in cells treated with etoposide [1]. When the function of SIRT1 is inhibited by EX527 or its expression is suppressed by RNAi, the upregulated level and release of IL-1β and TNF-α by high glucose are further increased [2]. When HCT116 cells were cultured in 0.1% serum, addition of EX-527 caused a 90% increase in cell number after 7 days. In the presence of 10% serum, EX-527 did not change cell number in long term culture [3]. |
体内活性 | The central pretreatment with Ex527 blunted the ghrelin-induced food intake in rats. Mice lacking p53, a target of SIRT1 action, failed to respond to ghrelin in feeding behavior. Ghrelin failed to phosphorylate hypothalamic AMPK when rats were pretreated with Ex527, as it did in p53 KO mice [4]. EX-527 abolished RSV-induced attenuation of microvascular inflammation in ob/ob septic mice [5]. |
细胞实验 | NCI-H460 cells, MCF-7 cells, U-2 OS cells, or HMEC were plated at 2,000 cells per well in opaque-walled 96-well plates for the viability assay and 800 cells per well in 96-well Cytostar-T scintillating microplates for the proliferation assay. Cells were incubated for 1 day (NCI-H460) or 2 days (MCF-7, U-2 OS, and HMEC) prior to exposure to DNA-damaging agents and deacetylase inhibitors. All experiments were performed in triplicate. For viability assays, cells were treated with the indicated compounds for 48 h. Cell viability was then determined using the Cell Titer-Glo luminescent assay, which measures total ATP levels as an index of cell number. Luminescence was measured on a Luminoskan Ascent. For the proliferation assay, 0.5 μCi/ml of [14C]thymidine was added to the medium immediately after the genotoxins and deacetylase inhibitors. Plates were counted at 48 h (HMEC) or 72 h (NCI-H460, MCF-7, and U-2 OS cells) in a Microbeta liquid scintillation counter. Thymidine incorporated by the cells was detected by proximity to the scintillant in the base of the Cytostar-T tissue culture plate [1]. |
动物实验 | Mice were injected with RSV (RSV) 30mg/kg (4ml/kg) or equivalent volume of DMSO (Vehicle) (4ml/kg) intraperitoneally 18 hours pre-sepsis. This dose of RSV in mice was as per documented literature. In one group of mice, RSV pre-treated mice received EX-527 (10 mg/kg intraperitoneally; 4ml/kg, Vehicle: DMSO) within 10 minutes of cecal ligation and puncture [5]. |
别名 | EX-527, 司来司他, SEN0014196 |
分子量 | 248.71 |
分子式 | C13H13ClN2O |
CAS No. | 49843-98-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 18.7 mg/mL (75 mM)
Ethanol: 12.4 mg/mL (50 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 4.0207 mL | 20.1037 mL | 40.2075 mL | 100.5187 mL |
5 mM | 0.8041 mL | 4.0207 mL | 8.0415 mL | 20.1037 mL | |
10 mM | 0.4021 mL | 2.0104 mL | 4.0207 mL | 10.0519 mL | |
20 mM | 0.201 mL | 1.0052 mL | 2.0104 mL | 5.0259 mL | |
50 mM | 0.0804 mL | 0.4021 mL | 0.8041 mL | 2.0104 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。
Selisistat 49843-98-3 Chromatin/Epigenetic DNA Damage/DNA Repair Sirtuin mammalian Huntington's inhibit pathology EX-527 Drosophila 司来司他 deacetylation SEN-0014196 EX 527 SEN0014196 Inhibitor SEN 0014196 disease EX527 inhibitor