Powder: -20°C for 3 years | In solvent: -80°C for 2 years
Selisistat S-enantiomer 是一种选择性的SIRT1抑制剂，IC50值为 98 nM。
| 产品描述 | Selisistat S-enantiomer is an effective and specific SIRT1 inhibitor (IC50 = 98 nM) and shows >200-fold selectivity against SIRT2/3. |
| 靶点活性 | SIRT1:98 nM |
| 体外活性 | Treatment with Selisistat S-enantiomer 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 Selisistat S-enantiomer 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 Selisistat S-enantiomer 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 Selisistat S-enantiomer caused a 90% increase in cell number after 7 days. In the presence of 10% serum, Selisistat S-enantiomer did not change cell number in long term culture [3]. |
| 体内活性 | The central pretreatment with Selisistat S-enantiomer 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 Selisistat S-enantiomer, as it did in p53 KO mice [4]. Selisistat S-enantiomer abolished RSV-induced attenuation of microvascular inflammation in ob/ob septic mice [5]. |
| 别名 | (1S)-6-氯-2,3,4,9-四氢-1H-咔唑-1-甲酰胺, EX-527 S-enantiomer, EX-527 (S-enantiomer) |
| 分子量 | 248.71 |
| 分子式 | C13H13ClN2O |
| CAS No. | 848193-68-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
DMSO: 20 mg/mL
Ethanol: 5 mg/mL
( < 1 mg/mL refers to the product slightly soluble or insoluble )
参考文献
剂量换算对于不同动物的给药剂量换算，您也可以参考 更多...
体内实验配液计算器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。
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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 S-enantiomer 848193-68-0 Chromatin/Epigenetic DNA Damage/DNA Repair Sirtuin Selisistat Senantiomer (1S)-6-氯-2,3,4,9-四氢-1H-咔唑-1-甲酰胺 EX-527 S-enantiomer (S)-Selisistat EX-527 (S-enantiomer) Selisistat S enantiomer inhibit Inhibitor inhibitor
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