2. Epigenetics PI3K/Akt/mTOR
  3. AMPK
  4. MK8722

MK8722 is a potent and systemic pan-AMPK activator.

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CAS 番号 : 1394371-71-1

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>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 99 在庫あり
Solution
10 mM * 1 mL in DMSO USD 99 在庫あり
Solid
5 mg $90 在庫あり
10 mg $150 在庫あり
25 mg $320 在庫あり
50 mg $540 在庫あり
100 mg $950 在庫あり
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カスタマーレビュー

Based on 24 publication(s) in Google Scholar

MK8722 関連抗体

Top Publications Citing Use of Products

    MK8722 purchased from MedChemExpress. Usage Cited in: Nat Metab. 2024 Aug;6(8):1529-1548.  [Abstract]

    Western blot analysis of PHGDH and AMPK pathway proteins in lysates of MDA-MB-231 cells treated for 48 h with the AMPK activator MK8722 (0-100 μM).

    MK8722 purchased from MedChemExpress. Usage Cited in: Nat Metab. 2024 Aug;6(8):1529-1548.  [Abstract]

    Sensitivity of MDA-MB-231, BT-549, and Hs 578T cells to CB-839 treatment after 24 h pre-treatment with 50 μM MK8722 to activate the adaptive AMPK signaling axis.

    MK8722 purchased from MedChemExpress. Usage Cited in: Nat Metab. 2024 Aug;6(8):1529-1548.  [Abstract]

    Western blot analysis of PHGDH and AMPK pathway proteins in lysates of MDA-MB-231 cells treated with 50 μM MK8722 for the indicated durations (0-48 h).

    MK8722 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 May 24;14(1):2994.  [Abstract]

    Western blot analysis of PHGDH and AMPK pathway proteins in lysates of MDA-MB-231 cells treated with 50 μM MK8722 for the indicated durations (0-48 h).

    MK8722 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 May 24;14(1):2994.  [Abstract]

    MK8722 (60 mg/kg; ip) inhibited Torin1-induced autophagy in the liver and gastrocnemius muscle of mice.

    AMPK アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    NUAK1 NUAK2 AMPK AMPK α1β1γ1 AMPK α2β1γ1 AMPK α1β2γ1 AMPK α2β2γ1 BRSK1 BRSK2 HUNK AMPKα

    • 生物活性

    • プロトコル

    • 純度とドキュメンテーション

    • 参考文献

    • カスタマーレビュー

    製品説明

    MK8722 is a potent and systemic pan-AMPK activator.

    IC50 & Target[1]

    AMPK

     

    Cellular Effect
    Cell Line Type Value Description References
    Sf9 EC50
    0.0014 μM
    Compound: 32; MK-8722
    Activation of rat hepatocytes AMPK alpha1/beta1/gamma1 expressed in baculovirus infected Sf9 cells
    Activation of rat hepatocytes AMPK alpha1/beta1/gamma1 expressed in baculovirus infected Sf9 cells
    		[PMID: 31930920]
    Sf9 EC50
    0.0075 μM
    Compound: 32; MK-8722
    Activation of rat hepatocytes AMPK alpha1/beta2/gamma1 expressed in baculovirus infected Sf9 cells
    Activation of rat hepatocytes AMPK alpha1/beta2/gamma1 expressed in baculovirus infected Sf9 cells
    		[PMID: 31930920]
    Sf9 EC50
    1 nM
    Compound: MK-8722
    Activation of recombinant human AMPK expressed in Sf9 cells using SAMS peptide as substrate preincubated for 30 mins followed by substrate addition and measured after 60 mins by fluorescence based assay
    Activation of recombinant human AMPK expressed in Sf9 cells using SAMS peptide as substrate preincubated for 30 mins followed by substrate addition and measured after 60 mins by fluorescence based assay
    		[PMID: 31358465]
    Sf9 EC50
    1 nM
    Compound: MK-8722
    Activation of recombinant mouse AMPK expressed in Sf9 cells using SAMS peptide as substrate preincubated for 30 mins followed by substrate addition and measured after 60 mins by fluorescence based assay
    Activation of recombinant mouse AMPK expressed in Sf9 cells using SAMS peptide as substrate preincubated for 30 mins followed by substrate addition and measured after 60 mins by fluorescence based assay
    		[PMID: 31358465]
    Sf9 EC50
    1 nM
    Compound: MK-8722
    Activation of recombinant rhesus monkey AMPK expressed in Sf9 cells using SAMS peptide as substrate preincubated for 30 mins followed by substrate addition and measured after 60 mins by fluorescence based assay
    Activation of recombinant rhesus monkey AMPK expressed in Sf9 cells using SAMS peptide as substrate preincubated for 30 mins followed by substrate addition and measured after 60 mins by fluorescence based assay
    		[PMID: 31358465]
    体外実験

    MK8722 (MK-8722) is a potent, direct, allosteric activator of all 12 mammalian AMPK complexes. MK8722 activates pAMPK complexes with increased potency and magnitude versus AMP, with EC50 values of ~1 to 60 nM and increased activation by factors of ~4 to 24. Although MK8722 exhibits higher affinity for β1-containing (~1 to 6 nM) versus β2-containing (~15 to 63 nM) pAMPK complexes, it is the most potent activator of β2 complexes reported to date. pAMPK activation by maximal AMP plus MK8722 is synergistic, demonstrating that the agents act at distinct sites[1].

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

    MK8722 関連抗体
    体内実験

    Chronic antihyperglycemic efficacy of MK8722 (MK-8722) is evaluated in db/db mice, a leptin receptor-deficient T2DM model. Once-daily administration of MK8722 results in dose-dependent lowering of ambient blood glucose. On treatment day 12, glucose reductions after MK8722 treatment (30 mpk/day) are comparable to those observed with the PPARγ agonist BRL49653 (3 mpk/day). Unlike BRL49653, the glucose-lowering action of MK8722 manifests without significant effects on body weight, which is a consistent finding. Dose-dependent increases in tissue pACC are maintained throughout the dosing period. Chronic efficacy, without tachyphylaxis, is also observed in additional dysmetabolic and diabetic rodent models. In all cases, efficacy is associated with trough MK8722 plasma levels comparable to the concentrations required to acutely stimulate skeletal muscle glucose uptake. Chronic MK8722 dosing in mice also increases muscle Glut4 protein levels, possibly contributing to efficacy[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    分子量

    449.89

    分子式

    C24H20ClN3O4
    CAS 番号
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O[C@H]1[C@@]([C@]2([H])OC1)([H])OC[C@H]2OC3=NC4=NC(C(C=C5)=CC=C5C6=CC=CC=C6)=C(Cl)C=C4N3
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : 31.25 mg/mL (69.46 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.2228 mL 11.1138 mL 22.2277 mL
    5 mM 0.4446 mL 2.2228 mL 4.4455 mL
    10 mM 0.2223 mL 1.1114 mL 2.2228 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

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

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始）

    C1

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    体積 （開始）

    V1

    =
    濃度 （終了）

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    体積 （終了）

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    体内:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: 2.08 mg/mL (4.62 mM); Clear solution; Need ultrasonic

      This protocol yields a clear solution of 2.08 mg/mL.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.08 mg/mL (4.62 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

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    (per animal)

    g

    Dosing volume
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    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
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    % 
    +
    %
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    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    純度とドキュメンテーション

    純度: 99.82%

    COA (249 KB) HNMR (295 KB) RP-HPLC (267 KB) MS (69 KB)

    取扱説明書 (2659 KB)
    参考文献
    動物実験
    [1]

    Mice[1]
    Housing Lean C57BL/6 mice at 10-12 weeks of age and C57BL/6 eDIO mice at 16 weeks of age are used. db/db mice at 7 weeks of age are used. Animals are maintained on a 12 hr/12 hr light-dark cycle with free access to food and water with the temperature maintained at 22ºC. Four lean C57BL/6 mice are housed in a standard cage. eDIO mice are individually caged. Eight db/db mice are housed in a large rodent cage. C57BL/6 mice and db/db mice are maintained on regular rodent chow diet 7012 (5% dietary fat; 3.75 kcal/g) for 1-2 weeks before receiving compound treatments. eDIO mice are maintained on 60% kcal% fat diet. Oral dosing of MK8722 in standard vehicle, or vehicle alone, is performed using 10 mL/kg body weight. The effect of MK8722 on various metabolic parameters is established by comparison to vehicle treated animals[1].

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    参考文献

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.2228 mL 11.1138 mL 22.2277 mL 55.5691 mL
    5 mM 0.4446 mL 2.2228 mL 4.4455 mL 11.1138 mL
    10 mM 0.2223 mL 1.1114 mL 2.2228 mL 5.5569 mL
    15 mM 0.1482 mL 0.7409 mL 1.4818 mL 3.7046 mL
    20 mM 0.1111 mL 0.5557 mL 1.1114 mL 2.7785 mL
    25 mM 0.0889 mL 0.4446 mL 0.8891 mL 2.2228 mL
    30 mM 0.0741 mL 0.3705 mL 0.7409 mL 1.8523 mL
    40 mM 0.0556 mL 0.2778 mL 0.5557 mL 1.3892 mL
    50 mM 0.0445 mL 0.2223 mL 0.4446 mL 1.1114 mL
    60 mM 0.0370 mL 0.1852 mL 0.3705 mL 0.9262 mL
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    MK8722 Related Classifications

    • Molarity Calculator

    • Dilution Calculator

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    The dilution calculator equation

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

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
    × = ×
    C1   V1   C2   V2
    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:

    MK87221394371-71-1MK 8722MK-8722AMPKAMP-activated protein kinaseInhibitorinhibitorinhibit

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    製品名:
    MK8722
    製品番号:
    HY-111363
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