Powder: -20°C for 3 years | In solvent: -80°C for 1 year
AK-7 是一种大脑可渗透的 SIRT2 抑制剂,可在神经元模型中表征其降低胆固醇的特性,IC50 为 15.5 μM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 245 | 现货 | ||
2 mg | ¥ 349 | 现货 | ||
5 mg | ¥ 567 | 现货 | ||
10 mg | ¥ 863 | 现货 | ||
25 mg | ¥ 1,690 | 现货 | ||
50 mg | ¥ 2,730 | 现货 | ||
100 mg | ¥ 3,990 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 689 | 现货 |
产品描述 | AK-7 is a brain-permeable SIRT2 inhibitor and to characterize its cholesterol-reducing properties in neuronal models with an IC50 of 15.5 μM. |
靶点活性 | SIRT2:15.5 μM |
体外活性 | AK-7 is a selective cell- and brain-permeable SIRT2 inhibitor,this SIRT2 inhibitor stimulated cytoplasmic retention of sterol regulatory element binding protein-2 and subsequent transcriptional downregulation of cholesterol biosynthesis genes, resulting in reduced total cholesterol in primary striatal neurons. Furthermore, the identified inhibitor reduced cholesterol in cultured na?ve neuronal cells and brain slices from wild-type mice[1].AK-7 has roles in metabolic diseases, cancer, age-related disorders, and neurodegenerative diseases, potentially including Alzheimer's, Huntington's, and Parkinson's diseases[2][3]. |
体内活性 | AK-7 (15 mg/kg/dose, i.p.) is brain-permeable in wild-type and HD mice[1]. |
激酶实验 | Sirtuin activity was assessed using the Fleur de Lys assay with recombinant active enzymes SIRT1, SIRT2, and the catalytically active fragment of SIRT3. Results were measured using a Multilabel plate reader (excitation 355 nm, emission 460 nm). Assays were performed using the manufacturer's recommendations, and each compound concentration was tested in triplicate. For each experiment, SIRT1 activity was normalized to 1 U/reaction well and SIRT2 and SIRT3 activity to 5 U/reaction well (where U = 1 pmol/min at 37 °C, 250 μM substrate, 500 μM NAD+). Each reaction well-contained enzyme, 500 μM NAD+, 250 μM fluorogenic deacetylase substrate, supplied reaction buffer, and the compound of interest or mock control (DMSO) in a total volume of 50 μL. Autofluorescent backgrounds were measured in triplicate in reaction solutions containing substrate, buffer, and NAD+ in triplicate and subtracted from experimental signals [1]. |
细胞实验 | Neuronal nuclear antigen (NeuN)-positive neurons and some astroglia were derived from mechanically dissociated ganglionic eminences of E16 rat embryos. The HD model based on the expression of mutant huntingtin has been described previously. Treatments of cultures with AK-7 were at 10 μM for 24 h unless stated otherwise. DMSO was included at the same concentrations as a control. Lower dose, chronic treatments with AK-7 were introduced to neurons at DIV4 and continued weekly coinciding with normal medium change [1]. |
动物实验 | AK-7, solubilized at 1.5 mg/mL in 25% Cremophor EL (BASF)/ 10% DMSO in water, was administered by intraperitoneal injection to 11 week old mice at 15 mg/kg/dose. Blood was collected and centrifuged at 7,000 rpm for 7 min, and then serum was aspirated and immediately frozen in liquid nitrogen. Brains were immediately frozen in liquid nitrogen and stored at -80 C. Brains were weighed and then homogenized in four volumes of 10% Cremophor RH40 in water using homogenizer, and 2% v/v phosphoric acid was added to the homogenate, vortexed, and centrifuged at 10,000g at 25 C for 1 h. The supernatant was aspirated, and solid phase extraction was performed immediately. Serum samples were vortexed into 2% v/v phosphoric acid and centrifuged at 2500 rpm for 10 min[1] |
分子量 | 437.35 |
分子式 | C19H21BrN2O3S |
CAS No. | 420831-40-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (114.32 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.2865 mL | 11.4325 mL | 22.865 mL | 57.1625 mL |
5 mM | 0.4573 mL | 2.2865 mL | 4.573 mL | 11.4325 mL | |
10 mM | 0.2286 mL | 1.1432 mL | 2.2865 mL | 5.7162 mL | |
20 mM | 0.1143 mL | 0.5716 mL | 1.1432 mL | 2.8581 mL | |
50 mM | 0.0457 mL | 0.2286 mL | 0.4573 mL | 1.1432 mL | |
100 mM | 0.0229 mL | 0.1143 mL | 0.2286 mL | 0.5716 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。
AK-7 420831-40-9 Chromatin/Epigenetic DNA Damage/DNA Repair Sirtuin AK7 AK 7 Inhibitor inhibit inhibitor