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- CAS号:
1093403-33-8
- 规格:
1mg/1g/5mg/10mg/25mg/50mg/100mg/200mg/500mg
| 规格: | 1mg | 产品价格: | ¥311.0 |
|---|---|---|---|
| 规格: | 1g | 产品价格: | ¥11920.0 |
| 规格: | 5mg | 产品价格: | ¥650.0 |
| 规格: | 10mg | 产品价格: | ¥1048.0 |
| 规格: | 25mg | 产品价格: | ¥1992.0 |
| 规格: | 50mg | 产品价格: | ¥3000.0 |
| 规格: | 100mg | 产品价格: | ¥4312.0 |
| 规格: | 200mg | 产品价格: | ¥6064.0 |
| 规格: | 500mg | 产品价格: | ¥8960.0 |
Product Introduction
Bioactivity
| 名称 | SRT 2104 |
| 描述 | SRT 2104 (GSK2245840) is a selective and brain-permeable SIRT1 activator. |
| 细胞实验 | Cells are cultured in low glucose Dulbecco's modified Eagle's medium (DMEM) supplemented with 10% fetal bovine serum and penicillin–streptomycin. Cells are treated with vehicle (0.1% DMSO) or 3?μM?SRT2104 for 24?h and then harvested for protein and Western blotting.(Only for Reference) |
| 激酶实验 | SIRT1 fluorescence polarization assay and HTS: In the SIRT1 FP assay, SIRT1 activity is monitored using a 20 amino acid peptide (Ac-Glu-Glu-Lys(biotin)-Gly-Gln-Ser-Thr-Ser-Ser-His-Ser-Lys(Ac)-Nle-Ser-Thr-Glu-Gly–Lys(MR121 or Tamra)-Glu-Glu-NH2 ) derived from the sequence of p53. The peptide is N-terminally linked to biotin and C-terminally modified with a fluorescent tag. The reaction for monitoring enzyme activity is a coupled enzyme assay where the first reaction is the deacetylation reaction catalyzed by SIRT1 and the second reaction is cleavage by trypsin at the newly exposed lysine residue. The reaction is stopped and streptavidin is added in order to accentuate the mass differences between substrate and product. The fluorescence polarization reaction conditions are as follows: 0.5 μM peptide substrate, 150 μM βNAD +, 0-10 nM SIRT1, 25 mM Tris-acetate pH 8, 137 mM Na-Ac, 2.7 mM K-Ac, 1 mM Mg-Ac, 0.05% Tween-20, 0.1% Pluronic F127, 10 mM CaCl 2 , 5 mM DTT, 0.025% BSA, and 0.15 mM nicotinamide. The reaction is incubated at 37°C and stopped by addition of nicotinamide, and trypsin is added to cleave the deacetylated substrate. This reaction is incubated at 37 ℃ in the presence of 1 μM streptavidin. Fluorescent polarization is determined at excitation (650 nm) and emission (680 nm) wavelengths. |
| 体外活性 | SRT2104 在 C2C12 细胞中降低 p65/RelA 的乙酰化水平。[1] |
| 体内活性 | 在雄性C57BL/6J小鼠中,SRT2104(100 mg/kg,口服)延长了标准饮食喂养小鼠的平均寿命和最大寿命,并提高了运动协调能力、骨密度、胰岛素敏感性,并降低了炎症。SRT2104的短期治疗能在萎缩实验模型中保持骨骼和肌肉质量。[1] 在雄性N171-82Q HD小鼠中,包含0.5% SRT2104的饮食能有效穿透血脑屏障,减缓脑萎缩,改善运动功能,并延长生存期。[2] |
| 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 | Ethanol : < 1 mg/mL (insoluble or slightly soluble) 10% DMSO+90% Saline : 0.38 mg/mL (0.74 mM), Suspension. H2O : < 1 mg/mL (insoluble or slightly soluble) DMSO : 3.79 mg/mL (7.34 mM), Sonication is recommended. |
| 关键字 | SRT-2104 | SRT 2104 | Sirtuin | SIRT1 | Inhibitor | inhibit | GSK-2245840 | GSK 2245840 |
| 相关产品 | Selisistat | Fisetin | Nicotinamide riboside | Nicotinamide | Dihydrocoumarin | MDL-800 | Nicotinamide riboside malate | Sirtinol | JGB1741 | SIRT6-IN-5 | SIRT5 inhibitor 8 | MC3482 |
| 相关库 | Anti-Aging Compound Library |
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文献和实验网络 第十九章 杂环化合物和生物碱 杂环化合物在自然界分布很广,其数量几乎占已知有机化合物的三分之一,用途也很多。许多重要的物质如叶绿素、血红素、核酸以及临床应用的一些有显著疗效的天然药物和合成药物等,都含有杂环化合物的结构。生物碱多是中草药的有效成分,绝大多数是含氮的杂环化合物。本章内容与医学关系密切,具有重要意义。
分子中具有高能键的化合物。在生物体内主要有上式(Ⅰ)和(Ⅱ)两种结构的高能化合物。其作用为贮藏能量(例如 ATP、肌酸磷酸)和作为产生 ATP源的中间代谢产物(例如磷酸烯醇丙酮酸)以及合成反应的中间物质(例如酰基辅酶 A),在蛋白质的结构( conformation)变化周期的第一阶段上(例如钠钾 ATP酶的羧基磷酸中间体)也具有重要作用。多数高等化合物具有磷酸基,但也有例外。
由不同种元素组成的纯净物叫做化合物。化合物一般有固定的组成。化合物的组成一般可用化学式表示。化合物具有确定的物理性质和化学性质,不同于其组成元素的性质。化合物中的元素不能用简单的机械方法或物理方法分开,而必须用化学方法才能分离。
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