A-769662

製品コードS2697

A-769662化学構造

分子量(MW):360.39

A-769662は一種の有効的で、可逆なAMPK活性剤で、無細胞試験でEC50値が0.8 μMになって、GPPase/FBPaseの活性にほとんど役立ちません。

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JPY 30237.48 あり
JPY 21166.23 あり
JPY 38876.76 あり
JPY 67674.36 あり

カスタマーフィードバック(4)

  • Cells were treated with CP, DOXO, SRT1720 (100 nM), EX527 (100 nM), A769662 (10 μM) and Compound C (1 μM) under normoxic or hypoxic conditions for 48 hours, and then their viabilities were measured by MTT.

    Cancer Res 2014 74(1), 298-308. A-769662 purchased from Selleck.

    Eight- to 10-week-old Ldlr-/- mice fed a standard laboratory chow were fasted overnight, fed at 07:00 h for 2 h, and refasted at 09:00 h. Intraperitoneal injection of vehicle, GW1516 (3 mg/kg), or A-769662 (30 mg/kg) (n = 6/group) occurred at the beginning of the refasting period at 09:00 h. Immunoblots of AMPK and ACC in freeze-clamped liver lysates 90 min postinjection. Representative immunoblots with quantitations are shown. Asterisk (*) indicates significant difference between vehicle and treatment; Student's paired t-test (P < 0.05).

    J Lipid Res 2014 55(7), 1254-1266. A-769662 purchased from Selleck.

  • Concentration-dependent effect of synthetic AMPK stimulator, A-769662, applied for 10 min on phosphorylated α subunit of AMPK. AMPK inhibitor (compound C, CC) was added to some samples at 10 uM. **p < 0.01, ***p < 0.001 vs. sample without A-769662 by ANOVA and Tukey post hoc test.

    Pharmacol Res 2014 81, 34-43. A-769662 purchased from Selleck.

    Cultured PANC-1 pancreatic cancer cells were treated with vehicle (DMSO, 1%), 10 uM of belinostat (BS, for 2 h, 4 h and 6 h) or A-769662 (10 uM, 2 h), phospho- and total AMPK and ACC were detected by western blot, tubulin (loading control) was also tested. AMPK and ACC phosphorylation was quantified as described.

    Biochem Biophys Res Commun 2013 437(1), 1-6. A-769662 purchased from Selleck.

製品安全説明書

AMPK阻害剤の選択性比較

生物活性

製品説明 A-769662は一種の有効的で、可逆なAMPK活性剤で、無細胞試験でEC50値が0.8 μMになって、GPPase/FBPaseの活性にほとんど役立ちません。
ターゲット
AMPK [1]
(Cell-free assay)
Fatty acid synthesis [1]
(Cell-free assay)
0.8 μM(EC50) 3.2 μM
体外試験

A-769662 stimulates partially purified rat liver AMPK with EC50 with 0.8 μM. A-769662 activates AMPK purified from multiple tissues and species in a dose-responsive manner with modest variations in observed EC50s. EC50s determined for A-769662 using partially purified AMPK extracts from rat heart, rat muscle, or human embryonic kidney cells (HEKs) are 2.2 mM, 1.9 mM, or 1.1 mM, respectively. A 4 hours treatment of primary rat hepatocytes with A-769662 dose-dependently increases ACC phosphorylation, which correlated inhibition of fatty acid synthesis with IC50 of 3.2 μM. A-769662 also inhibits fatty acid sythesis in mouse hepatocytes with IC50 with 3.6 μM [1] A-769662 activates AMPK both allosterically and by inhibiting dephosphorylation of AMPK on Thr-172, similar to the effects of AMP. [2] A-769662 inhibits proteasomal function by an AMPK-independent mechanism. A-769662 affects the in vitro activity of purified 26S proteasomes but not the in vitro activity of purified 20S proteasomes. A-769662 has toxic effects on MEF cells. [3] A recent research shows A-769662 inhibited cell proliferation and DNA synthesis. [4]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
mouse hepatocytes M1e2[WZ2dmO2aX;uJIF{e2G7 NFH6fJUyKG2P NUPkcGxlTE2VTx?= NUW5VYc1cW6qaXLpeJMh\mG2dImgZYNq\CC|eX70bIV{cXNid3n0bEBKSzVyIH;mJFMvPiEQvF2= NHvHclUyPjd3M{W3Oi=>
rat hepatocytes NXrWOnllTnWwY4Tpc44h[XO|YYm= M4rvflEhdU1? MYrEUXNQ NUDsb|FJcW6qaXLpeJMh\mG2dImgZYNq\CC|eX70bIV{cXNid3n0bEBKSzVyIH;mJFMvPiEQvF2= NWOwcXNFOTZ5NUO1O|Y>
HEK293 M3\pcGtqdmG|ZTDhd5NigQ>? NICyVXAzODBizszN Mm\FSG1UVw>? M4OzXoFkfGm4YYTld{BmdmSxZ3Xuc5V{KEGPUFu= NEPuUJUyPzd{OEK0NS=>
CCL13 M3P2b2tqdmG|ZTDhd5NigQ>? NGHMS24zODBizszN NXTT[WtsTE2VTx?= M{fxWoFkfGm4YYTld{BmdmSxZ3Xuc5V{KEGPUFu= Mnz6NVc4Ojh{NEG=
MEFs MkW1SpVv[3Srb36gZZN{[Xl? MlLjN|AxKM7:TR?= MkHvSG1UVw>? NGLp[3BqdmirYnn0d{Bxem:2ZXHzc41idCCodX7jeIlwdiCkeTDhckBCVVCNLXnu[IVx\W6mZX70JI1m[2ijbnnzcS=> NVPPeG86OTh3OUO1PFQ>
epididymal clear cells NYTwR29bTnWwY4Tpc44h[XO|YYm= MVSyNFAh|ryP NIPjUlRFVVOR M{LBVolvcGmkaYTzJJRp\SCySD3t[YRq[XSnZDDWMWFVWGG|ZTDhZ4N2dXWuYYTpc44h[XRidHjlJIFxcWOjbDDt[Y1jemGwZR?= MkfnNVkzOTF7MUi=
3T3-L1 MmPzSpVv[3Srb36gZZN{[Xl? NXLrRWV2OS5{IH3N MVTEUXNQ MXnpcohq[mm2czCzWFMuVDFiQXTpdI9o\W6nc3nz MXqxPVQ5OzNyNB?=
3T3-L1 NX7lRVlqTnWwY4Tpc44h[XO|YYm= M2nNbFEvOiCvTR?= M4XLRWROW09? NWr5SXFvcW6qaXLpeJMhfGinIFX4dJJme3Orb36gc4YhSWSrcH;n[Y5me2m|UnXsZZRm\CCWcnHud4NzcXC2aX;uJGZi[3SxcoOgZY5lKE2jcnvldpM> M{fZNlE6PDh|M{C0
3T3-L1 NYnSfVhiTnWwY4Tpc44h[XO|YYm= MX2xMlIhdU1? MWPEUXNQ MlzobY5pcWKrdIOgUYl1d3SrYzDDcI9v[WxiRYjwZY5{cW:w NF;qZ|AyQTR6M{OwOC=>
3T3-L1 M{\IVoN6fG:2b4jpZ4l1gSCjc4PhfS=> MlHTNU4zKG2P MnX0SG1UVw>? M2K0ZYRm[3KnYYPld{BE\WyuIG\pZYJqdGm2eR?= NFHmZpoyQTR6M{OwOC=>
3T3-L1 MVLLbY5ie2ViYYPzZZk> MX2xMlIhdU1? NWXWOFdYTE2VTx?= MXvhZ5RqfmG2ZYOgRW1RUw>? MXKxPVQ5OzNyNB?=
L6 skeletal muscle cells NXTONmJlTnWwY4Tpc44h[XO|YYm= NYCzVmdPOjVyIN88US=> MoPISG1UVw>? M{XXN4FkfGm4YYTld{BCVVCNIIPp[45idGmwZzDwZZRpf2G7cx?= MYOxPVgzQDh|Nh?=
L6 skeletal muscle cells MYTGeY5kfGmxbjDhd5NigQ>? MYGyOVAh|ryP NULYeZduTE2VTx?= MVnpcohq[mm2czD0bIUhVmFtLVurMWFVWGG|ZTD0doFve3CxcoSgZYN1cX[rdImgZY5lKGOnbHygd5Vz\mGlZTDhZpVv\GGwY3W= NHv0R|cyQTh{OEizOi=>
MDA-MB231 M3XNRWFxd3C2b4Ppd{Bie3OjeR?= NYLaW2l4PDByIN88US=> M2LhV2ROW09? NXTTZWxie2Wwc3n0bZpmeyCqdX3hckBjemWjc4SgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hXFKDSVytbY5lfWOnZDDhdI9xfG:|aYO= NF;nbXcyQTh7NkS2PS=>
BT474 M{G1eGFxd3C2b4Ppd{Bie3OjeR?= NUKyPGl2PDByIN88US=> MVnEUXNQ M3X1T5NmdnOrdHn6[ZMhcHWvYX6gZpJm[XO2IHPhcoNmeiClZXzsJIxqdmW|IITvJHRTSUmOLXnu[JVk\WRiYYDvdJRwe2m| Mn\JNVk5QTZ2Nkm=
MCF7 NEj3NJdCeG:ydH;zbZMh[XO|YYm= NWHaZXVLPDByIN88US=> M3HUN2ROW09? MlS4d4Vve2m2aYrld{BpfW2jbjDidoVie3RiY3HuZ4VzKGOnbHygcIlv\XNidH:gWHJCUUxvaX7keYNm\CCjcH;weI9{cXN? NXLzd5cxOTl6OU[0Olk>
Mesenchymal stem cells MXHLbY5ie2ViYYPzZZk> MYSxNEDDvU1? NV3nTHBXTE2VTx?= NYHhUmJIcW6mdXPld{BiKHKxYoXzeEBidmRic4XzeIFqdmWmIFHNVGsh[WO2aY\heIlwdg>? M4nCcFI1OTB2OEe5
Mesenchymal stem cells MYLjfZRwfG:6aXPpeJkh[XO|YYm= NEOxUIEyODBiwsXN MVLEUXNQ NI[3O2Nl\WO{ZXHz[ZMhfGinIF3TR{Bxem:uaX\ldoF1cW:w MnTYNlQyODR6N{m=
MG-63 NF2wco9kgXSxdH;4bYNqfHliYYPzZZk> M136fFExKML3TR?= MWrEUXNQ NYT1cYNXcW6qaXLpeJMhUDKRMj3JcoR2[2WmIF;zeIVw[myjc4SgR4VtdCCGZXH0bC=> MYqyOFk3ODN4Mh?=
MC3T3-E1 MlzsZ5l1d3SxeHnjbZR6KGG|c3H5 M{XkSVExKML3TR?= M1vvcGROW09? NWXhTFJ2cW6qaXLpeJMhUDKRMj3JcoR2[2WmIF;zeIVw[myjc4SgR4VtdCCGZXH0bC=> MXeyOFk3ODN4Mh?=
MG-63 NIfscZpCeG:ydH;zbZMh[XO|YYm= M2fBcFExKML3TR?= MWDEUXNQ M1XpXZN2eHC{ZYPz[ZMhUDKRMj3JcoR2[2WmIF;zeIVw[myjc4SgR4VtdCCDcH;weI9{cXN? NV3RfGpwOjR7NkCzOlI>
MC3T3-E1 MoGzRZBweHSxc3nzJIF{e2G7 MVWxNEDDvU1? MWDEUXNQ NITseY1{fXCycnXzd4V{KEh{T{KtTY5lfWOnZDDPd5Rmd2KuYYP0JGNmdGxiQYDvdJRwe2m| NYS5ZotvOjR7NkCzOlI>
MG-63 M1O0UWZ2dmO2aX;uJIF{e2G7 NI\FR3AyOCEEtV2= NF7me5dFVVOR MUPhcIxmfmmjdHXzJHJQWyCjY3P1cZVt[XSrb36gZY5lKEGWUDDk[ZBt\XSrb36gZ4F2e2WmIHL5JGgzVzJ? MWWyOFk3ODN4Mh?=
MC3T3-E1 MlP1SpVv[3Srb36gZZN{[Xl? NGHsWo0yOCEEtV2= MlT0SG1UVw>? NF25UFBidGyndnnheIV{KFKRUzDhZ4N2dXWuYYTpc44h[W6mIFHUVEBl\XCuZYTpc44h[2G3c3XkJIJ6KEh{T{K= M1z3UVI1QTZyM{[y
MG-63 M4mzOmZ2dmO2aX;uJIF{e2G7 M3jGRlExKML3TR?= MnLxSG1UVw>? NXPEW5E6\mGlaXzpeIF1\XNiSELPNk1qdmS3Y3XkJIF2fG:yaHHnfUBi[3SrdnH0bY9v NIHrVZIzPDl4MEO2Ni=>
MC3T3-E1 MXzGeY5kfGmxbjDhd5NigQ>? NFHNeVUyOCEEtV2= NWPOcpFHTE2VTx?= NF7GO2Vn[WOrbHn0ZZRmeyCKMl:yMYlv\HWlZXSgZZV1d3CqYXf5JIFkfGm4YYTpc44> MWCyOFk3ODN4Mh?=
PC3 M3znPGtqdmG|ZTDhd5NigQ>? M2qxd|ExOCEEtV2= MmPWSG1UVw>? NUTRflh6fXC{ZXf1cIF1\XNidHjlJIxmfmWuczDv[kBCVVCNIHHu[EBCS0NicHjvd5Bpd3K7bHH0bY9v MYeyOVU6PDB2Mx?=
PC3M NUPkN20yU2mwYYPlJIF{e2G7 NVjEfJh2OTByINM1US=> MVrEUXNQ MWD1dJJm\3WuYYTld{B1cGVibHX2[Yx{KG:oIFHNVGsh[W6mIFHDR{BxcG:|cHjvdplt[XSrb36= MXmyOVU6PDB2Mx?=
PC3 MVzGeY5kfGmxbjDhd5NigQ>? MYqxNFAhyrWP NVjxcW9tTE2VTx?= MlPTbY5lfWOnczDQTVNMN22WT2KgdIF1cHejeYO= MVqyOVU6PDB2Mx?=
PC3M M4TUPWZ2dmO2aX;uJIF{e2G7 NImwVXEyODBiwsXN MVTEUXNQ M3ftWYlv\HWlZYOgVGk{Uy:vVF;SJJBifGi5YYnz MY[yOVU6PDB2Mx?=
PC3 NWPFO|duT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NVvOfIxJOTByINM1US=> NGfHSoxFVVOR MXrzeZBxemW|c3XzJJBzd2yrZnXyZZRqd25? NYi0T4dpOjV3OUSwOFM>
PC3M MVnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NUTkfFdzOTByINM1US=> M3jDZ2ROW09? MXzzeZBxemW|c3XzJJBzd2yrZnXyZZRqd25? M3fFbVI2PTl2MESz
MC3T3-E1 MWLLbY5ie2ViYYPzZZk> NYDhZmVuOTBizszN NEfM[|ZFVVOR NEK4S4hqdmS3Y3XzJJNq\26rZnnjZY51KEGPUFugZYN1cX[jdHnvci=> M4XIUFI3QDlzOE[2
MC3T3-E1 MlPoS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MX2xNEDPxE1? MnfNSG1UVw>? MoexbY5pcWKrdIOgSIV5NWmwZIXj[YQhd3O2ZX;icIF{fCClZXzsJIRm[XSq M2j6fFI3QDlzOE[2
MC3T3-E1 M1faU2Z2dmO2aX;uJIF{e2G7 Mn3tNVAh|ryP NFuzVGxFVVOR NFexXphqdmirYnn0d{BF\XhvaX7keYNm\CCxeHnkZZRqfmVic4Ty[ZN{ NIXBflgzPjh7MUi2Oi=>

多くの細胞株試験データを見る場合、クリックしてください

体内試験 Short-term treatment of normal Sprague Dawley rats with A-769662 decreases liver malonyl CoA levels and the respiratory exchange ratio, VCO2/VO2, indicating an increased rate of whole-body fatty acid oxidation. Treatment of ob/ob mice with 30 mg/kg b.i.d. A-769662 decreases hepatic expression of PEPCK, G6Pase, and FAS, lowers plasma glucose by 40%, reduced body weight gain and significantly decreases both plasma and liver triglyceride levels. [1]

お薦めの試験操作(参考用のみ)

キナーゼ試験:

[1]

+ 展開

96-well AMPK assay:

AMPK activity is measured by monitoring phosphorylation of the SAMS peptide substrate (20 mM in standard assays and 100 mM in additivity assays) following a previously described protocol (Anderson et al., 2004). To determine whether A-769662-induced AMPK activation occurs in a reversible manner, AMP or A-769662 are preincubated with rat liver AMPK for 10 minutes at 20 times standard assay concentrations prior to dilution and measurement of AMPK activity.
細胞試験:

[3]

+ 展開
  • 細胞株: MEF cells
  • 濃度: 300 μM
  • 反応時間: 24 hours
  • 実験の流れ:

    Cell viability of MEF cells treated or not with A-769662 is performed as follows: cells are harvested by trypsinization and incubated with 0.5 mg/mL RNase and 50 μg/mL propidium iodine at room temperature in the dark; cell viability is analyzed by flow cytometry using a FACScanto flow cytometer, using an excitation laser at 488 nm and a propidium iodine fluorescence detection at 600 nm. To determine the proportion of cells in each phase of the cell cycle, cells are harvested by trypsinization, collected by centrifugation, washed in PBS and fixed overnight in 80% ethanol at -20 °C. Subsequently, these fixed cells are centrifuged to remove the fixative and incubated for 20 minutes in the dark at room temperature in PBS containing 0.5 mg/mL RNase and 50 μg/mL propidium iodine. Flow cytometry analysis is performed as above. The proportion of cells in G1, S, and G2 is determined using the MODFIT program. Cell culture pictures are taken at the indicated times using a camera coupled to an inverted microscope with a 20 × objective.


    (参考用のみ)
動物試験:

[1]

+ 展開
  • 動物モデル: Sprague Dawley rats
  • 製剤: A-769662 is dissolved in DMSO.
  • 投薬量: 30 mg/kg
  • 投与方法: Administered via i.p.
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 72 mg/mL (199.78 mM)
Water Insoluble
Ethanol Insoluble
体内 順序で溶剤を入れること:
1% DMSO+30% polyethylene glycol+1% Tween 80
30 mg/mL

* 溶解度検測はSelleck技術部門によって行いますので、文献より提供された溶解度と差異がある可能性がありますが、生産工芸と不同ロット(lot)で起きる正常な現象ですから、ご安心ください。

化学情報

分子量 360.39
化学式

C20H12N2O3S

CAS No. 844499-71-4
保管
in solvent
別名 N/A

便利ツール

モル濃度計算器

モル濃度計算器

解決のために必要とされるマス、ボリュームまたは濃度を計算してください。

マス (g) = 濃度 (mol/L) x ボリューム (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • マス
    濃度
    ボリューム
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備することを要求される希釈剤を計算してください. セレック希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 輸入 輸出 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • 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):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

マス 濃度 ボリューム 分子量

技術サポート

ストックの作り方、阻害剤の保管する方法、細胞実験や動物実験に注意すべきな点を全部含めており、製品を取扱う時よくあった質問に対して取扱説明書でお答えいたします。

Handling Instructions

他の質問がある場合は、お気軽くお問合せください。

  • * 必須

AMPK信号経路図

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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID