A-769662

目录号:S2697

仅限科研使用

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。

A-769662 Chemical Structure

CAS: 844499-71-4

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
大包装 有超大折扣
大剂量询单有大折扣!

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客户使用Selleck生产的A-769662发表文献60篇:

产品安全说明书

AMPK抑制剂选择性比较

相关AMPK产品

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 MWfGeY5kfGmxbjDhd5NigQ>? MknsNUBuVQ>? NWroXHlWTE2VTx?= NWHubVY4cW6qaXLpeJMh\mG2dImgZYNq\CC|eX70bIV{cXNid3n0bEBKSzVyIH;mJFMvPiEQvF2= MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPjd3M{W3Okc,OTZ5NUO1O|Y9N2F-
rat hepatocytes MWnGeY5kfGmxbjDhd5NigQ>? NV21WGdYOSCvTR?= MVzEUXNQ NWLJXHdscW6qaXLpeJMh\mG2dImgZYNq\CC|eX70bIV{cXNid3n0bEBKSzVyIH;mJFMvPiEQvF2= NGGxW5g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNke1N|U4Pid-MU[3OVM2PzZ:L3G+
HEK293 NFK5ZnRMcW6jc3WgZZN{[Xl? M1zhZ|IxOCEQvF2= NYjqXZZITE2VTx?= M4PiUYFkfGm4YYTld{BmdmSxZ3Xuc5V{KEGPUFu= M17KblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5N{K4NlQyLz5zN{eyPFI1OTxxYU6=
CCL13 M2OxWmtqdmG|ZTDhd5NigQ>? MlTONlAxKM7:TR?= M17JOWROW09? M1HCcoFkfGm4YYTld{BmdmSxZ3Xuc5V{KEGPUFu= MlHXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd5MkiyOFEoRjF5N{K4NlQyRC:jPh?=
MEFs M1\qW2Z2dmO2aX;uJIF{e2G7 NGG3N4E{ODBizszN M{TXTmROW09? M{XEcYlvcGmkaYTzJJBzd3SnYYPvcYFtKG[3bnP0bY9vKGK7IHHuJGFOWEtvaX7k[ZBmdmSnboSgcYVkcGGwaYPt NFfPZZY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEW5N|U5PCd-MUi1PVM2QDR:L3G+
epididymal clear cells M2n3SmZ2dmO2aX;uJIF{e2G7 NW\JZVh1OjByIN88US=> MnjDSG1UVw>? NIfLdm9qdmirYnn0d{B1cGVicFitcYVlcWG2ZXSgWk1CXFCjc3WgZYNkfW23bHH0bY9vKGG2IITo[UBieGmlYXygcYVu[nKjbnW= Ml7tQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl{MUG5NVgoRjF7MkGxPVE5RC:jPh?=
3T3-L1 M2nhb2Z2dmO2aX;uJIF{e2G7 NVfmPZlMOS5{IH3N MUXEUXNQ MX;pcohq[mm2czCzWFMuVDFiQXTpdI9o\W6nc3nz M4PU[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7NEizN|A1Lz5zOUS4N|MxPDxxYU6=
3T3-L1 NXuwOoF7TnWwY4Tpc44h[XO|YYm= MmDnNU4zKG2P MX3EUXNQ MWnpcohq[mm2czD0bIUhTXiycnXzd4lwdiCxZjDB[Ilxd2enbnXzbZNT\WyjdHXkJHRz[W6|Y4LpdJRqd25iRnHjeI9zeyCjbnSgUYFzc2W{cx?= NIP1V2U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUS4N|MxPCd-MUm0PFM{ODR:L3G+
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L6 skeletal muscle cells M1HOVmZ2dmO2aX;uJIF{e2G7 NXLqXYp5OjVyIN88US=> M2S3TmROW09? M3Tm[IFkfGm4YYTld{BCVVCNIIPp[45idGmwZzDwZZRpf2G7cx?= NITKfmg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUiyPFg{Pid-MUm4Nlg5OzZ:L3G+
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MDA-MB231 NHP0NG1CeG:ydH;zbZMh[XO|YYm= NVqzcmhLPDByIN88US=> NGS1eZJFVVOR M2r4OpNmdnOrdHn6[ZMhcHWvYX6gZpJm[XO2IHPhcoNmeiClZXzsJIxqdmW|IITvJHRTSUmOLXnu[JVk\WRiYYDvdJRwe2m| M4XDWVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OEm2OFY6Lz5zOUi5OlQ3QTxxYU6=
BT474 NYC5cpM2SXCxcITvd4l{KGG|c3H5 MkXzOFAxKM7:TR?= Mo\zSG1UVw>? M4TmWJNmdnOrdHn6[ZMhcHWvYX6gZpJm[XO2IHPhcoNmeiClZXzsJIxqdmW|IITvJHRTSUmOLXnu[JVk\WRiYYDvdJRwe2m| M1zaUFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OEm2OFY6Lz5zOUi5OlQ3QTxxYU6=
MCF7 MnG4RZBweHSxc3nzJIF{e2G7 M3v3OFQxOCEQvF2= NEG4[o1FVVOR M3TjcZNmdnOrdHn6[ZMhcHWvYX6gZpJm[XO2IHPhcoNmeiClZXzsJIxqdmW|IITvJHRTSUmOLXnu[JVk\WRiYYDvdJRwe2m| M4XFVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OEm2OFY6Lz5zOUi5OlQ3QTxxYU6=
Mesenchymal stem cells Mn7YT4lv[XOnIHHzd4F6 MVixNEDDvU1? M{fs[GROW09? MmmybY5lfWOnczDhJJJw[nW|dDDhcoQhe3W|dHHpcoVlKEGPUFugZYN1cX[jdHnvci=> MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDFyNEi3PUc,OjRzMES4O|k9N2F-
Mesenchymal stem cells MmXvZ5l1d3SxeHnjbZR6KGG|c3H5 NVLKcmpKOTByINM1US=> Mo\6SG1UVw>? Mn7D[IVkemWjc3XzJJRp\SCPU1OgdJJwdGmoZYLheIlwdg>? NVjLc3dkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSxNFQ5PzlpPkK0NVA1QDd7PD;hQi=>
MG-63 MlfRZ5l1d3SxeHnjbZR6KGG|c3H5 M1vhcFExKML3TR?= NIL0d2pFVVOR NF:wZlRqdmirYnn0d{BJOk9{LVnu[JVk\WRiT4P0[Y9jdGG|dDDD[YxtKESnYYTo NFLCV3Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEm2NFM3Oid-MkS5OlA{PjJ:L3G+
MC3T3-E1 M4\kOoN6fG:2b4jpZ4l1gSCjc4PhfS=> NHrOdFMyOCEEtV2= NYLmfJFTTE2VTx?= M3\lfYlvcGmkaYTzJGgzVzJvSX7keYNm\CCRc4Tlc4Jt[XO2IFPlcIwhTGWjdHi= M{Lod|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OU[wN|YzLz5{NEm2NFM3OjxxYU6=
MG-63 MUnBdI9xfG:|aYOgZZN{[Xl? NYTiUIRvOTBiwsXN MXPEUXNQ MVHzeZBxemW|c3XzJGgzVzJvSX7keYNm\CCRc4Tlc4Jt[XO2IFPlcIwhSXCxcITvd4l{ M1j3OFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OU[wN|YzLz5{NEm2NFM3OjxxYU6=
MC3T3-E1 NF20c2RCeG:ydH;zbZMh[XO|YYm= NVP3R|FXOTBiwsXN NG[1bm5FVVOR NEf2WGt{fXCycnXzd4V{KEh{T{KtTY5lfWOnZDDPd5Rmd2KuYYP0JGNmdGxiQYDvdJRwe2m| NFzTcZU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEm2NFM3Oid-MkS5OlA{PjJ:L3G+
MG-63 NHjWPGNHfW6ldHnvckBie3OjeR?= MVixNEDDvU1? NH;rS5JFVVOR MkjKZYxt\X[rYYTld{BTV1NiYXPjeY12dGG2aX;uJIFv\CCDVGCg[IVxdGW2aX;uJINifXOnZDDifUBJOk9{ NXnheHdRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5OlA{PjJpPkK0PVYxOzZ{PD;hQi=>
MC3T3-E1 MlP5SpVv[3Srb36gZZN{[Xl? MVGxNEDDvU1? NGf6XppFVVOR NWjMPFM3[WyuZY\pZZRmeyCUT2OgZYNkfW23bHH0bY9vKGGwZDDBWHAh\GWybHX0bY9vKGOjdYPl[EBjgSCKMl:y NIjhdHA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEm2NFM3Oid-MkS5OlA{PjJ:L3G+
MG-63 MWXGeY5kfGmxbjDhd5NigQ>? MU[xNEDDvU1? M2rjU2ROW09? NHTQ[Y9n[WOrbHn0ZZRmeyCKMl:yMYlv\HWlZXSgZZV1d3CqYXf5JIFkfGm4YYTpc44> MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDl4MEO2Nkc,OjR7NkCzOlI9N2F-
MC3T3-E1 M3m3c2Z2dmO2aX;uJIF{e2G7 M3i0clExKML3TR?= Mne5SG1UVw>? NULsOpFL\mGlaXzpeIF1\XNiSELPNk1qdmS3Y3XkJIF2fG:yaHHnfUBi[3SrdnH0bY9v MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDl4MEO2Nkc,OjR7NkCzOlI9N2F-
PC3 M1P1[WtqdmG|ZTDhd5NigQ>? NF:3Z2UyODBiwsXN M2\ZdmROW09? NHP5NYZ2eHKnZ4XsZZRmeyC2aHWgcIV3\Wy|IH;mJGFOWEtiYX7kJGFESyCyaH;zdIhwenmuYYTpc44> NIqzVZg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUW5OFA1Oyd-MkW1PVQxPDN:L3G+
PC3M NEfiTWFMcW6jc3WgZZN{[Xl? NFrxSHkyODBiwsXN NUnMfWc1TE2VTx?= NXXZVXdlfXC{ZXf1cIF1\XNidHjlJIxmfmWuczDv[kBCVVCNIHHu[EBCS0NicHjvd5Bpd3K7bHH0bY9v NXL2T2xiRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW1PVQxPDNpPkK1OVk1ODR|PD;hQi=>
PC3 NEW2c3lHfW6ldHnvckBie3OjeR?= NFTCfG0yODBiwsXN NUXkNnVWTE2VTx?= M{\1T4lv\HWlZYOgVGk{Uy:vVF;SJJBifGi5YYnz M2ntd|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NUm0NFQ{Lz5{NUW5OFA1OzxxYU6=
PC3M M3nRcWZ2dmO2aX;uJIF{e2G7 MlzQNVAxKML3TR?= M37FSGROW09? MmTjbY5lfWOnczDQTVNMN22WT2KgdIF1cHejeYO= MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTV7NEC0N{c,OjV3OUSwOFM9N2F-
PC3 MnvDS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MVKxNFAhyrWP NXjsc2hlTE2VTx?= NYLzRpkze3WycILld5NmeyCycn;sbYZmemG2aX;u MonJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV3OUSwOFMoRjJ3NUm0NFQ{RC:jPh?=
PC3M M2nlZ2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M2nHZVExOCEEtV2= M2LG[2ROW09? MYLzeZBxemW|c3XzJJBzd2yrZnXyZZRqd25? NWn4UmJVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW1PVQxPDNpPkK1OVk1ODR|PD;hQi=>
MC3T3-E1 MkG2T4lv[XOnIHHzd4F6 NVfPOlN[OTBizszN M4HWVmROW09? NGC5R5FqdmS3Y3XzJJNq\26rZnnjZY51KEGPUFugZYN1cX[jdHnvci=> NGHnPXQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nki5NVg3Pid-Mk[4PVE5PjZ:L3G+
MC3T3-E1 MnTrS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NYSwPYZVOTBizszN M{P0fGROW09? NYL1UZhrcW6qaXLpeJMhTGW6LXnu[JVk\WRib4P0[Y9jdGG|dDDj[YxtKGSnYYTo NVzPeoN[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[4PVE5PjZpPkK2PFkyQDZ4PD;hQi=>
MC3T3-E1 NGDBb|NHfW6ldHnvckBie3OjeR?= M2S4elExKM7:TR?= NFW0cXdFVVOR NF;6cI1qdmirYnn0d{BF\XhvaX7keYNm\CCxeHnkZZRqfmVic4Ty[ZN{ NEnpRoQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nki5NVg3Pid-Mk[4PVE5PjZ:L3G+
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Assay
Methods Test Index PMID
Western blot pCofilin / Cofilin / detyrosinated alpha tubulin / acetylated alpha tubulin p-AMPK / AMPK / p-S6K / S6K / p-ACC 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]

  • 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]

  • 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。
动物实验:

[1]

  • Animal Models: Sprague Dawley大鼠
  • Dosages: 30 mg/kg
  • Administration: 腹腔注射给药

溶解度(25°C)

体外

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 3年 -20°C 粉状
2年 -80°C 溶于溶剂

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)

mg/kg g μL

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
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

摩尔浓度计算器

质量 浓度 体积 分子量

技术支持

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操作手册

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