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AK-7

产品编号 T5490 CAS 420831-40-9

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。

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AK-7, CAS 420831-40-9

规格	价格/CNY	货期
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

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

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

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 50 mg/mL (114.32 mM)

溶液配制表

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

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Taylor DM, et al. A brain-permeable small molecule reduces neuronal cholesterol by inhibiting activity of sirtuin 2 deacetylase. ACS Chem Biol. 2011 Jun 17;6(6):540-6. 2. Machado D O R , Jana S , Kazantsev A G , et al. SIRT2 as a Therapeutic Target for Age-Related Disorders[J]. Frontiers in Pharmacology, 2012, 3. 3. Fridén-Saxin, Maria, Seifert T , Landergren, Marie Rydén, et al. Synthesis and Evaluation of Substituted Chroman-4-one and Chromone Derivatives as Sirtuin 2-Selective Inhibitors[J]. Journal of Medicinal Chemistry, 2012, 55(16):7104-7113.

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。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 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 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

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。

Keywords

AK-7 420831-40-9 Chromatin/Epigenetic DNA Damage/DNA Repair Sirtuin AK7 AK 7 Inhibitor inhibit inhibitor

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AK-7

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

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