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A-769662

A-769662 是一种可逆 AMPK 激活剂,EC50 值为 0.8 μM。具有代谢调控、抗肿瘤、抗炎等生物活性。可用于代谢与肿瘤药物研发。

CAS号

844499-71-4

分子式

C20H12N2O3S

主要靶点

Fatty Acid Synthase|AMPK

仅限科研使用

Cat No : CM02681

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Synonyms

AMP-activated protein kinase|AMPK|A769662|A-769662|A 769662|FAS|FattyAcidSynthase|Fatty Acid Synthase|inhibit|Inhibitor



产品信息

A-769662 is a reversible AMPK activator with an EC50 value of 0.8 μM. A-769662 exhibits biological activities including metabolic regulation, antitumor effects, and anti-inflammatory properties. A-769662 can be used in metabolic and oncology drug research and development.

CAS号 844499-71-4
分子式 C20H12N2O3S
主要靶点 Fatty Acid Synthase|AMPK
主要通路 表观遗传|PI3K/Akt/mTOR 信号通路|代谢
分子量 360.39
纯度 98.36%, 此纯度可做参考,具体纯度与批次有关系,可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.
别名 AMP-activated protein kinase|AMPK|A769662|A-769662|A 769662|FAS|FattyAcidSynthase|Fatty Acid Synthase|inhibit|Inhibitor

靶点活性

AMPK:0.8 μM(EC50)

体内活性

方法:雄性 BALB/c 小鼠腹腔注射 LPS 2 mg/kg,4 小时后腹腔注射 A-769662 10 mg/kg,8 小时后处死小鼠。 结果:A-769662 显著降低 Tlr-4 mRNA、MyD88 蛋白、TNF-α/IL-6 水平,同时增加 p-AMPK 和 p-ACC 水平。[2]

体外活性

方法:小鼠 BMSCs 加入 10 μM A-769662,处理 6 天,分时间点检测,Western blot 检测 p-AMPKα (Thr172) 和 p-ACC (Ser79)。 结果:A-769662 显著增加 AMPKα及其底物 ACC 的磷酸化水平,确认激活 AMPK 信号。[1]

溶解度

Ethanol:3.61 mg/mL (10.02 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:4.5 mg/mL (12.49 mM);DMSO:51 mg/mL (141.51 mM)

细胞实验

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)

参考文献

1.Abdallah BM, Alzahrani AM. A-769662 stimulates the differentiation of bone marrow-derived mesenchymal stem cells into osteoblasts via AMP-activated protein kinase-dependent mechanism. J Appl Biomed. 2021 Sep;19(3):159-169.
2.Rameshrad M, Maleki-Dizaji N, Soraya H, Toutounchi NS, Barzegari A, Garjani A. Effect of A-769662, a direct AMPK activator, on Tlr-4 expression and activity in mice heart tissue. Iran J Basic Med Sci. 2016 Dec;19(12):1308-1317.
3.Moreno D, et al, FEBS Lett, 2008, 583(17), 2650-2654.
4.Pevton KJ, et al, J Pharmacol Exp Ther, 2012, Jun 13.
5.Lu X Y, Shi X J, Hu A, et al. Feeding induces cholesterol biosynthesis via the mTORC1–USP20–HMGCR axis[J]. Nature. 2020, 588(7838): 479-484.

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