2. Epigenetics PI3K/Akt/mTOR
  3. AMPK
  4. A-769662

A-769662 是一种 AMP 活化蛋白激酶 (AMPK) 激活剂。A-769662 通过 AMPK 非依赖机制抑制 26S 蛋白酶体的功能，导致细胞周期停滞。A-769662 可直接刺激部分纯化的大鼠肝脏 AMPK (EC50 = 0.8 μM)，并抑制原代大鼠肝细胞中的脂肪酸合成 (IC50 = 3.2 μM)。A-769662 可以缓解 2 型糖尿病等代谢性疾病的症状。

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A-769662 Chemical Structure

A-769662 Chemical Structure

CAS No. : 844499-71-4

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥792
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5 mg ￥720
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10 mg ￥1246
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50 mg ￥3464
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100 mg ￥5350
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A-769662 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 36 篇科研文献

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    A-769662 purchased from MCE. Usage Cited in: Mol Cell. 2017 Oct 19;68(2):336-349.e6.  [Abstract]

    AMPK DKO SV40-immortalized MEFs are electroporated with plasmids encoding Myc-tagged AMPK α1, Myc-tagged AMPK α2 and Myc-tagged AMPK α2 S > A. 48 hr later, MEFs are starved for 3 hr and treated for 2 hr with DMSO or 50 mM A769662 before protein extraction. Western blot analysis shows the A769662-induced ACC phosphorylation in transfected cells.

    A-769662 purchased from MCE. Usage Cited in: Mol Neurobiol. 2017 Apr;54(3):2301-2312.  [Abstract]

    Effect of A769662 on high glucose-induced inflammatory changes in N2A cells and inflammatory marker expression in sciatic nerves of STZ induced rats. Representative immunoblot images of iNOS, COX-2, NF-κB, β-actin and corresponding graphical representations of densitometric analysis.

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    NUAK1 NUAK2 AMPK AMPK α1β1γ1 AMPK α2β1γ1 AMPK α1β2γ1 AMPK α2β2γ1

    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    A-769662 is a AMP-activated protein kinase (AMPK) activator. A-769662 inhibits the function of the 26S proteasome by an AMPK-independent mechanism and leads to cell cycle arrest. A-769662 directly stimulates partially purified rat liver AMPK (EC50 = 0.8 μM) and inhibits fatty acid synthesis in primary rat hepatocytes (IC50 = 3.2 μM). A-769662 can alleviate the symptoms of metabolic diseases such as type 2 diabetes[1][2][3][4].

    IC50 & Target[1]

    AMPK

    0.8 μM (EC50)

    细胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    Hepatocyte IC50
    3.2 μM
    Compound: 2, A-769662
    Activation of AMPK in rat primary hepatocytes assessed as inhibition of fatty acid biosynthesis by 14C-acetate incorporation assay
    Activation of AMPK in rat primary hepatocytes assessed as inhibition of fatty acid biosynthesis by 14C-acetate incorporation assay
    		[PMID: 24900695]
    体外研究
    (In Vitro)

    A-769662 (0.1-100 μM) increases AMPK activity in the presence of a saturating concentration of AMP (300 μM)[1].
    A-769662 (1 nM-1 mM, 4h) increases acetyl-CoA carboxylase (ACC) phosphorylation dose-dependently in primary rat hepatocytes[1].
    A-769662 (50-300 μM, 1 h) increases the GFP-dependent fluorescence dose-dependently in HEK-GFPu-1 cells[3].
    A-769662 (0-50 μM, 1 h) is able to reduce the activity of pre-existing proteasomal activity in MEF cells[3].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    A-769662 相关抗体:

    Western Blot Analysis[1]

    Cell Line: Primary rat hepatocytes
    Concentration: Primary rat hepatocytes
    Incubation Time: 4 h
    Result: Increased ACC phosphorylation dose-dependently.
    Showed that increased ACC phosphorylation correlated with inhibition of fatty acid synthesis as measured by incorporation of 14C-acetate into fatty acids with IC50 of 3.2 μM.
    体内研究
    (In Vivo)

    A-769662 (30 mg/kg，腹腔注射，单剂量) 显著降低了相对于载体的呼吸交换率，表明尽管 Sprague Dawley 大鼠体内有碳水化合物，但脂肪酸利用率仍增加[1]。
    A-769662 (3-30 mg/kg，腹腔注射，每日两次，共 5 天) 降低了肥胖/肥胖小鼠和瘦型同窝小鼠的血糖水平、脂质和 ACC 活性[1]。
    A-769662 (3-30 mg/kg，腹腔注射，每日两次，共 14 天) 降低了肥胖/肥胖小鼠和瘦型同窝小鼠的血糖水平[1]。
    A-769662 (10-300 μM，1 小时) 抑制在小鼠胚胎成纤维细胞 (MEF) 中，蛋白酶体功能显著增强，在野生型和双 α1 -/- α1 -/- KO 小鼠中的 IC50 为 62 μM[3]。
    A-769662 (300 μM) 对野生型和双 α1 -/- α1 -/- KO 小鼠的 MEF 细胞有毒性作用[3]。
    A-769662 (15-30 mg/kg，腹腔注射，2 周) 可诱导 AMPK 活化，从而使糖尿病小鼠的神经功能变化正常化，并减轻与糖尿病神经病变 (DN) 相关的疼痛[4]。

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: Sprague Dawley rats fed ad libitum prior were first acclimated by placing them in a gas exchange indirect calorimeter without food for 2 h then gavaged with a mixed meal plus A-769662[1]
    Dosage: 30 mg/kg
    Administration: Intraperitoneal injection (i.p.), single dose
    Result: Resulted in 33% reduction of malonyl CoA levels in livers of treated animals in relative to the vehicle.
    Had a statistically nonsignificant decrease in malonyl CoA levels in skeletal muscle of rats treated with A-769662.
    Animal Model: 6- to 7-weeks-old ob/ob and lean littermate mice[3]
    Dosage: 3 or 30 mg/kg b.i.d. for 5 days; 3, 10, or 30 mg/kg b.i.d. for 14 days
    Administration: Intraperitoneal injection (i.p.)
    Result: Significantly decreases fed plasma glucose (30-40% reduction) at 30 mg/kg in both 5 d and 14 d studies.
    Reduced 42% of the fed glucose levels (16 h postdose) in the 5 day study.
    Resulted in a modest reduction in body weight gain in ob/ob mice treated with 30 mg/kg dose for 5 days.
    Resulted in a transient reduction in food intake in the 14 d study.
    Increased the compound concentrations in liver 1 h after 30 or 3 mg/kg of A-769662 approximately 30-fold or 2.5-fold above the cellular IC50 for fatty acid synthesis.
    Animal Model: Healthy male Sprague-Dawley rats (250-270 g) fed on standard diet and water ad libitum then induced diabetes with Streptozotocin (HY-13753) (55 mg/kg, i.p.)[4]
    Dosage: 15 or 30 mg/kg for 14 days
    Administration: Intraperitoneal injection (i.p.)
    Result: Attenuated the pain hypersensitivity and resulted in improved tail flick latencies and paw withdrawal threshold.
    Resulted in marked reduction in motor/sensory nerve conduction velocities (MNCV and SNCV) as well as restoring impaired nerve blood flow (NBF).
    Significantly reduced TUNEL-positive cells, inhibited the lipid peroxidation and improved the antioxidant defence by improving glutathione levels in the sciatic nerves of treated diabetes rats.
    Significantly reduces the expression of IL-6 and TNF-α and reduced the expression of NF-κB and COX-2 compared to diabetic rats.
    Reversed AMPK inactivation and associated mitochondrial biogenesis and autophagy deficits in diabetic rats.
    Significantly elevated mitochondrial ATP production in treated rats.
    分子量

    360.39

    Formula

    C20H12N2O3S
    CAS 号
    性状

    固体

    颜色

    Off-white to yellow

    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性数据
    细胞实验： 

    DMSO 中的溶解度 : 50 mg/mL (138.74 mM; 超声助溶 (<80°C); 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.7748 mL 13.8739 mL 27.7477 mL
    5 mM 0.5550 mL 2.7748 mL 5.5495 mL
    查看完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
    储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    动物实验：

    请根据您的 实验动物和给药方式 选择适当的溶解方案。

    以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
    ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
    以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

    • 方案 一

      请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (6.94 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

      生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
    • 方案 二

      请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (6.94 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。

      2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
    动物溶解方案计算器
    请输入动物实验的基本信息：

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    只
    由于实验过程有损耗，建议您多配一只动物的量
    请输入您的动物体内配方组成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。
    您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
    连续给药周期超过半月以上，请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
    纯度 & 产品资料

    纯度: 99.33%

    COA (296 KB) HNMR (288 KB) RP-HPLC (282 KB) MS (69 KB)

    产品使用指南 (1538 KB)
    参考文献

    A-769662 相关分类

    完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
    储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.7748 mL 13.8739 mL 27.7477 mL 69.3693 mL
    5 mM 0.5550 mL 2.7748 mL 5.5495 mL 13.8739 mL
    10 mM 0.2775 mL 1.3874 mL 2.7748 mL 6.9369 mL
    15 mM 0.1850 mL 0.9249 mL 1.8498 mL 4.6246 mL
    20 mM 0.1387 mL 0.6937 mL 1.3874 mL 3.4685 mL
    25 mM 0.1110 mL 0.5550 mL 1.1099 mL 2.7748 mL
    30 mM 0.0925 mL 0.4625 mL 0.9249 mL 2.3123 mL
    40 mM 0.0694 mL 0.3468 mL 0.6937 mL 1.7342 mL
    50 mM 0.0555 mL 0.2775 mL 0.5550 mL 1.3874 mL
    60 mM 0.0462 mL 0.2312 mL 0.4625 mL 1.1562 mL
    80 mM 0.0347 mL 0.1734 mL 0.3468 mL 0.8671 mL
    100 mM 0.0277 mL 0.1387 mL 0.2775 mL 0.6937 mL
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    A-769662844499-71-4A769662A 769662AMPKAMP-activated protein kinase26S proteasomecell cycle arresttype 2 diabetesInhibitorinhibitorinhibit

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