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49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 MkPZSpVv[3Srb36gZZN{[Xl? NELye3EyKG2P M{DVfmROW09? NHzyN5ZqdmirYnn0d{Bn[XS2eTDhZ4llKHO7boTo[ZNqeyC5aYToJGlEPTBib3[gN{43KM7:TR?= MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPjd3M{W3Okc,OTZ5NUO1O|Y9N2F-
rat hepatocytes M4r2O2Z2dmO2aX;uJIF{e2G7 NU\Xd5djOSCvTR?= M1\GeGROW09? M{H5WolvcGmkaYTzJIZifHS7IHHjbYQhe3mwdHjld4l{KHerdHigTWM2OCCxZjCzMlYh|ryP MlHRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTZ5NUO1O|YoRjF4N{WzOVc3RC:jPh?=
HEK293 MWTLbY5ie2ViYYPzZZk> NYPzdnpNOjByIN88US=> MmTNSG1UVw>? MYHhZ5RqfmG2ZYOg[Y5ld2enbn;1d{BCVVCN MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzd{OEK0NUc,OTd5MkiyOFE9N2F-
CCL13 Ml25T4lv[XOnIHHzd4F6 NGq2dIEzODBizszN M2PiXWROW09? M3HvZ4FkfGm4YYTld{BmdmSxZ3Xuc5V{KEGPUFu= NXy1epI5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUe3NlgzPDFpPkG3O|I5OjRzPD;hQi=>
MEFs NFXUdnFHfW6ldHnvckBie3OjeR?= NV3ZR|dDOzByIN88US=> MWTEUXNQ M{PNZYlvcGmkaYTzJJBzd3SnYYPvcYFtKG[3bnP0bY9vKGK7IHHuJGFOWEtvaX7k[ZBmdmSnboSgcYVkcGGwaYPt NFzyVW49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEW5N|U5PCd-MUi1PVM2QDR:L3G+
epididymal clear cells NFv5fGxHfW6ldHnvckBie3OjeR?= M{LYdlIxOCEQvF2= NVixXXk4TE2VTx?= MVrpcohq[mm2czD0bIUheEhvbXXkbYF1\WRiVj3BWHBie2ViYXPjeY12dGG2aX;uJIF1KHSqZTDhdIlk[WxibXXtZpJidmV? NHL4dlE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUKxNVkyQCd-MUmyNVE6OTh:L3G+
3T3-L1 M3zxc2Z2dmO2aX;uJIF{e2G7 MWixMlIhdU1? MmLISG1UVw>? NFrXOGVqdmirYnn0d{A{XDNvTEGgRYRqeG:pZX7ld4l{ Mn;0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl2OEOzNFQoRjF7NEizN|A1RC:jPh?=
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L6 skeletal muscle cells M3Hnb2Z2dmO2aX;uJIF{e2G7 MmT2NlUxKM7:TR?= MUfEUXNQ NEm3dGtqdmirYnn0d{B1cGViTnGrMWssNUGWUHHz[UB1emGwc4DvdpQh[WO2aY\peJkh[W6mIHPlcIwhe3W{ZnHj[UBi[nWwZHHuZ4U> NYrLUYpHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm4Nlg5OzZpPkG5PFI5QDN4PD;hQi=>
MDA-MB231 NHnvboZCeG:ydH;zbZMh[XO|YYm= M{fWd|QxOCEQvF2= NXz1XYROTE2VTx?= NH;vWWp{\W6|aYTpfoV{KGi3bXHuJIJz\WG|dDDjZY5k\XJiY3XscEBtcW6nczD0c{BVWkGLTD3pcoR2[2WmIHHwc5B1d3Orcx?= NIPZe5M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUi5OlQ3QSd-MUm4PVY1Pjl:L3G+
BT474 MnfDRZBweHSxc3nzJIF{e2G7 MlzvOFAxKM7:TR?= Ml\QSG1UVw>? Mor1d4Vve2m2aYrld{BpfW2jbjDidoVie3RiY3HuZ4VzKGOnbHygcIlv\XNidH:gWHJCUUxvaX7keYNm\CCjcH;weI9{cXN? M1jhRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OEm2OFY6Lz5zOUi5OlQ3QTxxYU6=
MCF7 M{HHWWFxd3C2b4Ppd{Bie3OjeR?= M1PsT|QxOCEQvF2= NUDre2ZJTE2VTx?= M13lZZNmdnOrdHn6[ZMhcHWvYX6gZpJm[XO2IHPhcoNmeiClZXzsJIxqdmW|IITvJHRTSUmOLXnu[JVk\WRiYYDvdJRwe2m| M4TiWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OEm2OFY6Lz5zOUi5OlQ3QTxxYU6=
Mesenchymal stem cells M3zySGtqdmG|ZTDhd5NigQ>? M{LmWFExKML3TR?= NWHH[oRlTE2VTx?= MVrpcoR2[2W|IHGgdo9jfXO2IHHu[EB{fXO2YXnu[YQhSU2SSzDhZ5RqfmG2aX;u M{XxV|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MUC0PFc6Lz5{NEGwOFg4QTxxYU6=
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MG-63 NF\GW2FHfW6ldHnvckBie3OjeR?= M3rBelExKML3TR?= NGD5RopFVVOR MXnmZYNqdGm2YYTld{BJOk9{LXnu[JVk\WRiYYX0c5Bp[We7IHHjeIl3[XSrb36= NHe3S5o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEm2NFM3Oid-MkS5OlA{PjJ:L3G+
MC3T3-E1 MlLMSpVv[3Srb36gZZN{[Xl? NULZZ4xxOTBiwsXN NIrRPHpFVVOR NGe0Wm1n[WOrbHn0ZZRmeyCKMl:yMYlv\HWlZXSgZZV1d3CqYXf5JIFkfGm4YYTpc44> NUPsbWJ4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5OlA{PjJpPkK0PVYxOzZ{PD;hQi=>
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PC3M NEfjTJJHfW6ldHnvckBie3OjeR?= NYPBTXpzOTByINM1US=> MU\EUXNQ NFzsWZFqdmS3Y3XzJHBKO0txbWTPVkBx[XSqd3H5dy=> NHjGeGg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUW5OFA1Oyd-MkW1PVQxPDN:L3G+
PC3 MVrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NXrrbmZVOTByINM1US=> NVjmV41bTE2VTx?= MlTyd5VxeHKnc4Pld{Bxem:uaX\ldoF1cW:w M2jDU|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NUm0NFQ{Lz5{NUW5OFA1OzxxYU6=
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MC3T3-E1 NHO4eXZHfW6ldHnvckBie3OjeR?= NXq3bFA{OTBizszN M3r4OmROW09? Mn\BbY5pcWKrdIOgSIV5NWmwZIXj[YQhd3irZHH0bZZmKHO2cnXzdy=> NUPhXWJtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[4PVE5PjZpPkK2PFkyQDZ4PD;hQi=>
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PANC-08-13 Ml3IS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIrreFlKdmirYnn0bY9vKG:oIHj1cYFvKFCDTlOtNFguOTNiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OCB;IES3Mlk3PDFizszNMi=> MmXOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVEzPTB2Lze+V2FPT0WUPD;hQi=>
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D-336MG NITydJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{m1SmlvcGmkaYTpc44hd2ZiaIXtZY4hTC1|M{\NS{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwJF0hPDhwNEi0OUDPxE1w MnzGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVEzPTB2Lze+V2FPT0WUPD;hQi=>
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MCF7 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYfUdmxDUW6qaXLpeIlwdiCxZjDoeY1idiCPQ1[3JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUCgQUA1QS53OE[1JO69VS5? M{L3N|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFUyOjVyND:nQnNCVkeHUkyvZV4>
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YKG-1 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4nuRmlvcGmkaYTpc44hd2ZiaIXtZY4hYUuJLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3MDC9JFQ6Njl2MUKg{txONg>? MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1NVI2ODRxJ{7TRW5ITVJ:L3G+

... 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