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- 详细信息
- 文献和实验
- 技术资料
- 保存条件：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 保质期：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 英文名：
AK-7
- 库存：
现询
- 供应商：
北京索莱宝科技有限公司
- CAS号：
420831-40-9
- 规格：
50mg/25mg/1mg/10mg/5mg
| 规格： | 50mg | 产品价格： | ￥3245.0 |
|---|---|---|---|
| 规格： | 25mg | 产品价格： | ￥2090.0 |
| 规格： | 1mg | 产品价格： | ￥296.0 |
| 规格： | 10mg | 产品价格： | ￥1090.0 |
| 规格： | 5mg | 产品价格： | ￥677.0 |
AK 7是一种SIRT2抑制剂。
| 基本信息 | |
| CAS | No.420831-40-9 |
| 中文名称 | N-(3-溴苯基)-3-[(六氢-1H-氮杂卓-1-基)磺酰基]-苯甲酰胺 |
| 英文名称 | AK-7 |
| 别名 | N-(3-溴苯基)-3-[(六氢-1H-氮杂卓-1-基)磺酰基]-苯甲酰胺 |
| 分子式 | C19H21BrN2O3S |
| 分子量 | 437.35 |
| 溶解性 | Soluble in DMSO |
| 纯度 | ≥98% |
| 外观(性状) | White to off-white Solid |
| 储存条件 | Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| MDL | MFCD03140195 |
| SMILES | O=S(N1CCCCCC1)(C2=CC(C(NC3=CC(Br)=CC=C3)=O)=CC=C2)=O |
| InChIKey | IYAYHZZWYNXHEQ-UHFFFAOYSA-N |
| InChI | InChI=1S/C19H21BrN2O3S/c20-16-8-6-9-17(14-16)21-19(23)15-7-5-10-18(13-15)26(24,25)22-11-3-1-2-4-12-22/h5-10,13-14H,1-4,11-12H2,(H,21,23) |
| PubChem CID | 1328033 |
| 靶点 | SIRT2 |
| 通路 | Cell Cycle;DNA Damage/DNA Repair; Epigenetics |
| 背景说明 | AK 7是一种SIRT2抑制剂。 |
| 生物活性 | AK-7 is a selective cell- and brain-permeable SIRT2 inhibitor， with an IC50 of 15.5 μM.[1-3] |
| In Vitro | AK-7 (10 μM) reduces cholesterol levels in naive N2a neuroblastoma cells and hippocampal slice cultures from wild-type mice. AK-7 (1 μM) shows neuroprotective effect of AK-7 in striatal Huntington’s disease (HD) neurons[1]. AK-7 (12.5 μM) decreases ratio of DA neurons in primary midbrain cultures[3]. |
| 细胞实验 | AK-7 (15 mg/kg/dose， i.p.) is brain-permeable in wild-type and HD mice[1]. AK-7 (10， 20 mg/kg， i.p.) improves the behavior and neuropathological phenotype and extends survival of R6/2 HD mice. AK-7 (20 mg/kg) ameliorates HD neuropathology in R6/2 mice. AK-7 also reduces the polyglutamine aggregation in R6/2 brain. In addition， AK-7 treated 140CAG mice show motor performance changes that parallel untreated wild-type mice， with the 20 mg/kg dose being most effective and significantly different from untreated 140CAG mice[2]. |
| 细胞实验 | Neuronal nuclear antigen (NeuN)-positive neurons and some astroglia are derived from mechanically dissociated ganglionic eminences of E16 rat embryos. The HD model is based on the expression of mutant huntingtin. Treatments of cultures with AK-7 are at 10 μM for 24 h unless stated otherwise. DMSO is included at the same concentrations as a control. Lower dose， chronic treatments with AK-7 are 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， is administered by intraperitoneal injection to 11 week old mice at 15 mg/kg/dose， and compound levels in serum and brain are measured following sacrifice. Blood is collected and centrifuged at 7，000 rpm for 7 min， and then serum is aspirated and immediately frozen in liquid nitrogen. Brains are immediately frozen in liquid nitrogen and stored at ?80°C. Brains are weighed and then homogenized in four volumes of 10% Cremophor RH40 in water using a Polytron homogenizer， and 2% v/v phosphoric acid is added to the homogenate， vortexed， and centrifuged at 10，000 g at 25°C for 1 h. The supernatant is aspirated， and solid phase extraction is performed immediately. Serum samples are vortexed into 2% v/v phosphoric acid and centrifuged at 2500 rpm for 10 min[1]. |
| 数据来源文献 | [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]. Chopra V， et al. The sirtuin 2 inhibitor AK-7 is neuroprotective in Huntingtons disease mouse models. Cell Rep. 2012 Dec 27;2(6):1492-7. [3]. Szego EM， et al. Sirtuin 2 enhances dopaminergic differentiation via the AKT/GSK-3β/β-catenin pathway. Neurobiol Aging. 2017 Aug;56:7-16. |
| 单位 | 瓶 |
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文献和实验了样品的液流技术、细胞的分选和计数技术，以及数据的采集和分析技术等。 2.细胞的参量和荧光探针 FCM 是通过测量细胞的多种参量来获取信息的，细胞参数分为结构参量和功能参量两大类。结 构参量主要用于描述细胞的化学组分和形态特征，例如DNA、RNA的含量，总蛋白含量、胞内PH值 和细胞大小等；功能参量主要是描述细胞整体的理化和生物特性，如：细胞周期动力学、特殊配体的鉴 定、特殊细胞的生物活性等，这些参量有的需要经荧光标记才能被测定，有的并不需要荧光标记[4]。 2．1参数
A逆转录技术和PCR技术相结合的一种RNA指纹图谱技术。每一种细胞（包括同一组织细胞经过不同的处理）都有其特异表达的不同于其他组织细胞的基因谱（有差异基因表达），即特异的RNA指纹图谱。差异基因表达是细胞分化的基础，正是这些基因在细胞中的特异表达与否，决定了生命历程中细胞的发育和分化、细胞周期调节、细胞衰老和凋亡等。mRNA DDR T－PCR 技术正是对组织特异性表达基因进行分离的一种快速而行之有效的方法。 其基本原理是从基因背景相同的2个或几个被比较的细胞系或组织中提取总RNA，逆转录成cDNA
th e S ev en th A n n u a l S ym p o s iu m in B o ta n y , J a n u a r y 1 2 —1 4 , 1 9 8 4 ,U n ive r s ity o f C a lifo r n ia , R iv e r s id e (Dugger, W. M. and Bartnicki-Garcia, S., eds.),American Society of Plant Physiologists
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