A-769662

For research use only. Not for use in humans.

目录号:S2697

A-769662 Chemical Structure

CAS No. 844499-71-4

A-769662是一种有效的,可逆的AMPK激活剂,在无细胞试验中EC50为0.8 μM,对GPPase/FBPase活性几乎没有作用。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 1719.08 现货
RMB 1200.38 现货
RMB 3860.59 现货
RMB 10401.3 现货
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客户使用Selleck生产的A-769662发表文献45篇:

产品安全说明书

AMPK抑制剂选择性比较

生物活性

产品描述 A-769662是一种有效的,可逆的AMPK激活剂,在无细胞试验中EC50为0.8 μM,对GPPase/FBPase活性几乎没有作用。
靶点
AMPK [1]
(Cell-free assay)
Fatty acid synthesis [1]
(in primary rat hepatocytes)
0.8 μM(EC50) 3.2 μM
体外研究

A-769662部分刺激纯化的大鼠肝脏AMPK,EC50 为0.8 μM。A-769662以剂量响应的方式激活从多种组织和物种纯化得到的AMPK,伴随不同的EC50s。A-769662的EC50s,使用从大鼠心脏,大鼠肌肉,或人胚肾细胞(HEKs)部分纯化的AMPK测定,结果分别为2.2 mM,1.9 mM,或1.1 mM。原代大鼠肝细胞用A-769662处理4小时剂量依赖性增加ACC磷酸化,其与脂肪酸合成的抑制相关,IC50为3.2 μM。A-769662也会抑制小鼠肝细胞中脂肪酸合成,IC50为3.6 μM。[1] A-769662通过变构调节和抑制AMPK在Thr-172上的去磷酸化作用激活AMPK,类似于AMP的作用。[2] A-769662通过与AMPK无关的作用机制抑制蛋白酶体功能。 A-769662影响纯化26S蛋白酶体的体外活性,但是不影响纯化20S蛋白酶体的体外活性。A-769662对MEF细胞具有毒性作用。[3]一项最近的研究表明,A-769662抑制细胞增殖和DNA合成。[4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
mouse hepatocytes NX7KPWJjTnWwY4Tpc44h[XO|YYm= NFW5WlQyKG2P NF;pNm1FVVOR NW\XeXJbcW6qaXLpeJMh\mG2dImgZYNq\CC|eX70bIV{cXNid3n0bEBKSzVyIH;mJFMvPiEQvF2= M4\md|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF4N{WzOVc3Lz5zNke1N|U4PjxxYU6=
rat hepatocytes M2r1TmZ2dmO2aX;uJIF{e2G7 NGL0WlAyKG2P M{TmN2ROW09? Mk\ubY5pcWKrdIOg[oF1fHliYXPp[EB{gW62aHXzbZMhf2m2aDDJR|UxKG:oIEOuOkDPxE1? NFThUG49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNke1N|U4Pid-MU[3OVM2PzZ:L3G+
HEK293 NFrJdHFMcW6jc3WgZZN{[Xl? MVmyNFAh|ryP NH;ZZXVFVVOR NIXSOZZi[3SrdnH0[ZMh\W6mb3flco92eyCDTWDL NWP2OYxPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUe3NlgzPDFpPkG3O|I5OjRzPD;hQi=>
CCL13 MUTLbY5ie2ViYYPzZZk> NIDLbWszODBizszN NEja[IlFVVOR M2jST4FkfGm4YYTld{BmdmSxZ3Xuc5V{KEGPUFu= MkDjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd5MkiyOFEoRjF5N{K4NlQyRC:jPh?=
MEFs NXW1TZVuTnWwY4Tpc44h[XO|YYm= M1:3PFMxOCEQvF2= MYPEUXNQ Mkj2bY5pcWKrdIOgdJJwfGWjc3;tZYwh\nWwY4Tpc44h[nliYX6gRW1RUy2rbnTldIVv\GWwdDDt[YNp[W6rc32= MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDV7M{W4OEc,OTh3OUO1PFQ9N2F-
epididymal clear cells NHLrT5FHfW6ldHnvckBie3OjeR?= M1;rUlIxOCEQvF2= M1;XcWROW09? NXH0UmNIcW6qaXLpeJMhfGinIIDIMY1m\GmjdHXkJHYuSVSSYYPlJIFk[3WvdXzheIlwdiCjdDD0bIUh[XCrY3HsJI1mdWK{YX7l Mn[xQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl{MUG5NVgoRjF7MkGxPVE5RC:jPh?=
3T3-L1 NIfRW2xHfW6ldHnvckBie3OjeR?= NH\HR4cyNjJibV2= M{jtOWROW09? NUDKPHZzcW6qaXLpeJMhO1R|LVyxJGFlcXCxZ3Xu[ZNqew>? NV7qSpRSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm0PFM{ODRpPkG5OFg{OzB2PD;hQi=>
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L6 skeletal muscle cells NVvpOmRzTnWwY4Tpc44h[XO|YYm= MWGyOVAh|ryP MkXCSG1UVw>? NFy2eJNi[3SrdnH0[ZMhSU2SSzDzbYdv[WyrbnegdIF1cHejeYO= Mnu2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl6Mki4N|YoRjF7OEK4PFM3RC:jPh?=
L6 skeletal muscle cells MnrBSpVv[3Srb36gZZN{[Xl? M1n0ZVI2OCEQvF2= NXWyT3ZWTE2VTx?= MnvpbY5pcWKrdIOgeIhmKE6jKz3LL{1CXFCjc3WgeJJidnOyb4L0JIFkfGm4aYT5JIFv\CClZXzsJJN2em[jY3WgZYJ2dmSjbnPl MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTh{OEizOkc,OTl6Mki4N|Y9N2F-
MDA-MB231 MYXBdI9xfG:|aYOgZZN{[Xl? M4HOVlQxOCEQvF2= MknISG1UVw>? M2LjUJNmdnOrdHn6[ZMhcHWvYX6gZpJm[XO2IHPhcoNmeiClZXzsJIxqdmW|IITvJHRTSUmOLXnu[JVk\WRiYYDvdJRwe2m| MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTh7NkS2PUc,OTl6OU[0Olk9N2F-
BT474 NYnKNI45SXCxcITvd4l{KGG|c3H5 NX\WTW15PDByIN88US=> MoS2SG1UVw>? MVjz[Y5{cXSrenXzJIh2dWGwIHLy[YF{fCClYX7j[ZIh[2WubDDsbY5meyC2bzDUVmFKVC2rbnT1Z4VlKGGyb4D0c5Nqew>? MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTh7NkS2PUc,OTl6OU[0Olk9N2F-
MCF7 NUPURo04SXCxcITvd4l{KGG|c3H5 MkK3OFAxKM7:TR?= MV;EUXNQ NUL2UZBxe2Wwc3n0bZpmeyCqdX3hckBjemWjc4SgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hXFKDSVytbY5lfWOnZDDhdI9xfG:|aYO= NYTGR4xSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm4PVY1PjlpPkG5PFk3PDZ7PD;hQi=>
Mesenchymal stem cells MVnLbY5ie2ViYYPzZZk> NYXuPYZyOTBiwsXN MVLEUXNQ MnnTbY5lfWOnczDhJJJw[nW|dDDhcoQhe3W|dHHpcoVlKEGPUFugZYN1cX[jdHnvci=> MoDjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRzMES4O|koRjJ2MUC0PFc6RC:jPh?=
Mesenchymal stem cells NVrBeZBI[3m2b4TvfIlkcXS7IHHzd4F6 MYCxNFAhyrWP NGjiSZdFVVOR M3WwUoRm[3KnYYPld{B1cGViTWPDJJBzd2yrZnXyZZRqd25? NGHtPIE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEGwOFg4QSd-MkSxNFQ5Pzl:L3G+
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MC3T3-E1 Mn3nZ5l1d3SxeHnjbZR6KGG|c3H5 NUXKdGg5OTBiwsXN MlzsSG1UVw>? NUj1PYR5cW6qaXLpeJMhUDKRMj3JcoR2[2WmIF;zeIVw[myjc4SgR4VtdCCGZXH0bC=> NXz2XWlLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5OlA{PjJpPkK0PVYxOzZ{PD;hQi=>
MG-63 MlHtRZBweHSxc3nzJIF{e2G7 NHzHTJAyOCEEtV2= NH\BSGtFVVOR NY[zW2hpe3WycILld5NmeyCKMl:yMWlv\HWlZXSgU5N1\W:kbHHzeEBE\WyuIFHwc5B1d3Orcx?= MnW0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7NkCzOlIoRjJ2OU[wN|YzRC:jPh?=
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MG-63 NV\DNJE1TnWwY4Tpc44h[XO|YYm= MlnmNVAhyrWP MmnkSG1UVw>? NVfrNXVQ[WyuZY\pZZRmeyCUT2OgZYNkfW23bHH0bY9vKGGwZDDBWHAh\GWybHX0bY9vKGOjdYPl[EBjgSCKMl:y M2nDelxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OU[wN|YzLz5{NEm2NFM3OjxxYU6=
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MG-63 M1flRWZ2dmO2aX;uJIF{e2G7 NH\LVpAyOCEEtV2= Mnu3SG1UVw>? NHvUUW1n[WOrbHn0ZZRmeyCKMl:yMYlv\HWlZXSgZZV1d3CqYXf5JIFkfGm4YYTpc44> M2rPeVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OU[wN|YzLz5{NEm2NFM3OjxxYU6=
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PC3 NGCzWGFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NX\yXYF5OTByINM1US=> NXT5c3RQTE2VTx?= M2\zZ5N2eHC{ZYPz[ZMheHKxbHnm[ZJifGmxbh?= NY\kPHNTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW1PVQxPDNpPkK1OVk1ODR|PD;hQi=>
PC3M M4TWWWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MXGxNFAhyrWP MnviSG1UVw>? MXjzeZBxemW|c3XzJJBzd2yrZnXyZZRqd25? MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTV7NEC0N{c,OjV3OUSwOFM9N2F-
MC3T3-E1 NF\tO|VMcW6jc3WgZZN{[Xl? NUHIb|hXOTBizszN MkPZSG1UVw>? NF3PUW9qdmS3Y3XzJJNq\26rZnnjZY51KEGPUFugZYN1cX[jdHnvci=> MlXVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ6OUG4OlYoRjJ4OEmxPFY3RC:jPh?=
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MC3T3-E1 NF7VWIdHfW6ldHnvckBie3OjeR?= MkLYNVAh|ryP MVvEUXNQ NHfoTpZqdmirYnn0d{BF\XhvaX7keYNm\CCxeHnkZZRqfmVic4Ty[ZN{ MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjh7MUi2Okc,OjZ6OUG4OlY9N2F-
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YKG-1 M3jOOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4PWWGlvcGmkaYTpc44hd2ZiaIXtZY4hYUuJLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3MDC9JFQ6Njl2MUKg{txONg>? NIjiO2k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2OTJ3MESvK|5USU6JRWK8M4E,

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
pCofilin / Cofilin / detyrosinated alpha tubulin / acetylated alpha tubulin ; 

PubMed: 26431377     


A & B. MCF-7 cells were treated with 100–400 μM of A-769662 for 4-24 hours. Protein was harvested and Western blot analysis was done to determine levels of pAMPK at threonine 172, pCofilin at serine 3, detyrosinated alpha tubulin (glu-tub), and acetylated alpha tubulin (acetyl-tub). C & D. BT-549 cells were treated with 100–400 μM A-769662 for 4–24 hours. Protein was harvested and Western blot analysis was done to determine levels of markers listed above.

p-AMPK / AMPK / p-S6K / S6K / p-ACC ; 

PubMed: 22456226     


Representative immunoblots for p-AMPK, total AMPK, p-S6K, total S6K, p-ACC and actin under control conditions (C) and in response to 50 μM A-769662 at various time points.

26431377 22456226
体内研究 A-769662对正常Sprague Dawley大鼠的短期治疗降低肝脏丙二酰CoA水平,和换气比值,VCO2/VO2,表明整体脂肪酸氧化比率增加。A-769662(30 mg/kg, b.i.d.)治疗ob/ob小鼠,减少PEPCK,G6Pase,和FAS的肝脏表达,降低40%血浆葡萄糖,减少体重增加,并显著降低血浆和肝脏甘油三酯水平。[1]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:

[1]

- 合并

96-孔 AMPK 试验:

AMPK活性通过监测SAMS多肽底物(标准试验中为20 mM,附加试验中为100 mM)磷酸化根据前述方案(Anderson et al., 2004)测量。为测定 A-769662诱导的AMPK活化是否可逆,AMP或A-769662与大鼠肝脏AMPK在20倍标准试验浓度下预培养10分钟,然后稀释并测量AMPK活性。
细胞实验:

[3]

- 合并
  • Cell lines: MEF细胞
  • Concentrations: 300 μM
  • Incubation Time: 24小时
  • Method: A-769662处理或未处理的MEF细胞的细胞活性如下进行测定:细胞通过胰蛋白酶化采集,并与0.5 mg/mL RNase 和50 μg/mL碘化丙啶在室温下黑暗中进行培育;细胞活性通过流式细胞术使用FACScanto流式细胞分析仪分析,激发激光波长为488 nm,碘化丙啶荧光检测波长为600 nm。为测定细胞周期各阶段的细胞比例,细胞通过胰蛋白酶化采集,通过离心收集,用PBS洗涤,并在80%乙醇中于-20°C固定过夜。随后,将这些固定的细胞离心以除去固定剂,并于黑暗中,室温下,在包含0.5 mg/mL RNase 和50 μg/mL碘化丙啶的PBS中培养20分钟。流式细胞术分析如上进行。G1,S,和G2期的细胞比例使用MODFIT程序测定。细胞培养照片在指示时间使用结合具有20倍物镜的倒置显微镜的相机拍摄。
    (Only for Reference)
动物实验:

[1]

- 合并
  • Animal Models: Sprague Dawley大鼠
  • Dosages: 30 mg/kg
  • Administration: 腹腔注射给药
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 72 mg/mL (199.78 mM)
Water Insoluble
Ethanol Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
5% DMSO+40% PEG 300+5% Tween 80+50% ddH2O
5 mg/ml

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 360.39
化学式

C20H12N2O3S

CAS号 844499-71-4
储存条件 粉状
溶于溶剂
别名 N/A

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

技术支持

在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题,请给我们留言。

  • * 必填项

AMPK Signaling Pathway Map

相关AMPK产品

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID