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A-769662

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  • ¥1568
  • LC labs
  • 美国
  • A-1803
  • 2025年07月11日
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    • 详细信息
    • 文献和实验
    • 技术资料
    • 保存条件

      见说明书

    • 保质期

      >1年

    • 英文名

      A-769662

    • 库存

      期货2-3周

    • 供应商

      上海经科化学科技有限公司

    • CAS号

      844499-71-4

    • 规格

      10mg


    供应商:上海经科化学科技有限公司


    服务热线:400-0199-638


    QQ:472482400(上海经科)


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    本试剂(A-769662)
    仅供科研实验使用,不得用于其他用途!

    简介:
    货 号:A-1803
    名 称:A-769662
    别 名:A-769662
    C A S :844499-71-4
    分子量
    :360.39
    分子式:C20H12N2O3S
    纯 度:HPLC/TLC:>99%
    说 明:Storage: Store at or below -20 ºC. Solubility: Soluble in DMSO at 33 mg/mL; soluble in ethanol at 5 mg/mL with slight warming; very poorly soluble in water; maximum solubility in plain water is estimated to be about 50-100 µM; buffers, serum, or other additives may increase or decrease the aqueous sol. Disposal: A.
    文 献
    :A-769662 is a potent and reversible activator of AMP-activated protein kinase (AMPK). AMPK is an αβγ heterotrimer and plays an important role in regulating cellular and whole-body metabolism. A-769662 only activates AMPK heterotrimers containing the β1 subunit. A-769662 activates AMPK through the β subunit carbohydrate-binding module and the γ subunit but not the AMP-binding sites. Scott, J.W., et al. "Thienopyridone drugs are selective activators of AMP-activated protein kinase β1-containing complexes." Chem. Biological 15: 1220-1230 (2008). A-769662 stimulated partially purified rat liver AMPK with an EC50 of 0.8 µM and inhibited fatty acid synthesis in primary rat hepatocytes with an IC50 of 3.2 µM. A-769662 decreased liver malonyl CoA levels of Sprague Dawley rats and the respiratory exchange ratio, VCO2/VO2, and thus increased rate of whole-body fatty acid oxidation. A-769662 reduced hepatic expression of PEPCK, G6Pase, and FAS, decreased body weight gain, lowered plasma glucose by 40%, and reduced both plasma and liver triglyceride levels in ob/ob mice. Cool, B., et al. "Identification and characterization of a small molecule AMPK activator that treats key components of type 2 diabetes and the metabolic syndrome." Cell Metab. 3: 403-416 (2006). A-769662 induces allosteric activation of AMP-activated protein kinase (AMPK) and inhibition of dephosphorylation of AMPK on Thr-172, similar to the effects of AMP. Sanders, M.J., et al. "Defining the mechanism of activation of AMP-activated protein kinase by the small molecule A-769662, a member of the thienopyridone family." J. Biol. Chem. 282: 32539-32548 (2007). The effects of A-769662 are not dependent on the upstream kinase used in intact cells. Göransson, O., et al. "Mechanism of action of A-769662, a valuable tool for activation of AMP-activated protein kinase." J. Biol. Chem. 282: 32549-32560 (2007). In skeletal muscle, A-769662 activates β1-containing AMPK complexes, but induces glucose uptake via a PI3 kinase-dependent pathway. Treebak, J.T., et al. "A-769662 activates AMPK β1-containing complexes but induces glucose uptake through a PI3 kinase-dependent pathway in mouse skeletal muscle." Am. J. Physiol. Cell Physiol. 297: C1041-C1052 (2009). A-769662 inhibits 3T3-L1 adipocyte differentiation and may be used to treat obesity. Zhou, Y., et al. "Inhibitory effects of A-769662, a novel activator of AMP-activated protein kinase, on 3T3-L1 adipogenesis." Biol. Pharm. Bull. 32: 993-998 (2009). A-769662 inhibited the function of the 26S proteasome via an AMPK-independent mechanism. Moreno, D., et al. "A769662, a novel activator of AMP-activated protein kinase, inhibits non-proteolytic components of the 26S proteasome by an AMPK-independent mechanism." FEBS Lett. 582: 2650-2654 (2008). Sold for laboratory or manufacturing purposes only; not for human, medical, veterinary, food, or household use. This product is offered for R&D use in accordance with (i) 35 USC 271(e)+A13(1) in the U.S.; (ii) Section 69.1 of Japanese Patent Law in Japan; (iii) Section 11, No. 2 of the German Patent Act of 1981 in Germany; (iv) Section 60, Paragraph 5b of the U.K. Patents Act of 1977 in the U.K.; (v) Sections 55.2(1) and 55.2(6) and other common law exemptions of Canadian patent law; (vi) Section 68B of the Patents Act of 1953 in New Zealand together with the amendment of same by the Statutes Amendment Bill of 2002; (vii) such related legislation and/or case law as may be or become applicable in the aforementioned countries; and (viii) such similar laws and rules as may apply in various other countries.

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    图标文献和实验
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    • Cell专栏:没想到缺氧竟然也能抗衰老、提高化疗效果...

      磷酸化和 S6 激酶的高水平,但这种信号在低氧下培养的细胞中却不存在。 图片来源:Molecular Cell 上述的实验证明,低氧环境下的衰老细胞表现为 mTOR 通路的下调,而 mTOR 通路的抑制可由多种机制实现,包括 AMPK,一种在低氧环境中帮助维持能量平衡的传感器。此前有报道指出,二甲双胍是一种具有激活 AMPK 等多种分子功能的抗糖尿病药物,可降低常氧衰老细胞的 SASP。 因此,研究人员通过基因过表达或选择性 AMPK 激活剂 A769662 对细胞进行处理,结果发现,在常氧衰老

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