| 名稱 | A-769662 |
| 描述 | A-769662 is an effective, reversible AMPK activator(EC50=0.8 μM). |
| 細(xì)胞實(shí)驗(yàn) | 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. (Only for Reference) |
| 激酶實(shí)驗(yàn) | 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. |
| 體外活性 | 在ob/ob小鼠中,A-769662（30 mg/kg, b.i.d. ）,能夠減少PEPCK、G6Pase和FAS的肝臟表達(dá),降低血漿葡萄糖含量,降低血漿和肝臟中甘油三酯水平,從而減少體重的增加. |
| 體內(nèi)活性 | 在多種組織和物種純化得到的AMPK,均能夠被A-769662以劑量依賴的方式激活。對(duì)于AMPK來源于純化的大鼠肝臟（EC50=0.8 μM）大鼠心臟（EC50=2.2 mM）,大鼠肌肉（EC50=1.9 mM）,或人胚腎細(xì)胞(HEKs)（EC50=1.1 mM）。在肝細(xì)胞中,A-769662增加ACC磷酸化,抑制脂肪酸合成,原代大鼠肝細(xì)胞（IC50=3.2 μM）,小鼠肝細(xì)胞（IC50=3.6 μM）。通過抑制AMPK在Thr-172上的去磷酸化作用和變構(gòu)調(diào)節(jié),A-769662能夠激活A(yù)MPK。A-769662能夠抑制純化的26S蛋白酶體的體外活性。A-769662能夠抑制細(xì)胞增殖和DNA合成。 |
| 存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | Ethanol : 3.6 mg/mL (9.99 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 4.5 mg/mL (12.49 mM), Solution.
DMSO : 45 mg/mL (124.86 mM), Sonication is recommended.
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| 關(guān)鍵字 | Inhibitor | inhibit | FattyAcidSynthase | Fatty Acid Synthase | FAS | AMPK | AMP-activated protein kinase | A-769662 | A769662 |
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