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

A-769662 is a potent, reversible AMPK activator with EC50 of 0.8 μM.

For research use only. We do not sell to patients.

A-769662 Chemical Structure

A-769662 Chemical Structure

CAS No. : 844499-71-4

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 73 In-stock
Solution
10 mM * 1 mL in DMSO USD 73 In-stock
Solid
5 mg USD 66 In-stock
10 mg USD 92 In-stock
50 mg USD 330 In-stock
100 mg USD 594 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 31 publication(s) in Google Scholar

A-769662 Related Antibodies

Top Publications Citing Use of Products

29 Publications Citing Use of MCE A-769662

WB

    A-769662 purchased from MedChemExpress. 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 MedChemExpress. 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.

    View All AMPK Isoform Specific Products:

    View All Isoforms
    NUAK1 NUAK2 AMPK AMPK α1β1γ1 AMPK α2β1γ1 AMPK α1β2γ1 AMPK α2β2γ1

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    A-769662 is a potent, reversible AMPK activator with EC50 of 0.8 μM.

    IC50 & Target[1]

    AMPK

    0.8 μM (EC50)

    In Vitro

    A-769662 is equally potent in activating the baculovirus expressed α1,β1,γ1 recombinant isoform of AMPK (EC50=0.7 μM). A-769662 and A-592107 activate AMPK purified from multiple tissues and species in a dose-responsive manner with modest variations in observed EC50s. EC50s determined for A-769662 using partially purified AMPK extracts from rat heart, rat muscle, or human embryonic kidney cells (HEKs) are 2.2 μM, 1.9 μM, or 1.1 μM, respectively[1]. A-769662 activates endogenous AMPK in LKB1-expressing (HEK293) and LKB1-deficient (CCL13) cells. A-769662 allosterically activates AMPK complexes containing γ1 harboring a substitution of arginine residue 298 to glycine (R298G). A-769662 inhibits dephosphorylation of Thr-172 in the mutant γ1-containing complexes to a similar degree as seen in the wild-type complexes[2]. A769662 (300 μM) has toxic effects on MEF cells. A769662 reversibly inhibits the proteasomal activity[3].

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

    A-769662 Related Antibodies
    In Vivo

    A-769662 (30 mg/kg, i.p.) significantly reduced the respiratory exchange ratio (RER) in the SD rat. There are 33% and 58% reductions of malonyl CoA levels in livers of animals treated with 30 mg/kg A-769662 (0.905 nmol/g) or 500 mg/kg metformin (0.574 nmol/g), respectively. A-769662 (30 mg/kg, b.i.d.) significantly decreases fed plasma glucose (30%-40% reduction), while the lower doses (3 and 10 mg/kg) of A-769662 had no effect on the in diabetic ob/ob mice[1].

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

    360.39

    Formula

    C20H12N2O3S
    CAS No.
    Appearance

    Solid

    SMILES

    N#CC1C(C2=C(NC1=O)SC=C2C3=CC=C(C4=CC=CC=C4O)C=C3)=O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (138.74 mM; ultrasonic and warming and heat to 80°C; 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 2.7748 mL 13.8739 mL 27.7477 mL
    5 mM 0.5550 mL 2.7748 mL 5.5495 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

    • Dilution Calculator

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

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    In Vivo:

    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: ≥ 2.5 mg/mL (6.94 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (6.94 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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
    (per animal)

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    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    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.
    Purity & Documentation

    Purity: 99.20%

    COA (258 KB) LCMS (93 KB) Elemental Analysis Report (117 KB)

    Handling Instructions (2659 KB)
    References
    Kinase Assay
    [1]

    To assay glycogen phosphorylase b (GPb) activity, 1.5 μg/mL of rabbit GPb is added to a reaction mix containing 20 mM Na2HPO4 (pH 7.2), 2 mM MgSO4, 1 mM β-NADP (β-nicotinamide adenine dinucleotide phosphate), 1.4 U/mL G-6-PDH (Glucose-6-Phosphate-Dehydrogenase) and 3 U/mL PGM (phosphoglucomutase). AMP or test compounds are added to the assay medium at the specified concentrations followed by the addition of glycogen (final concentration 1 mg/mL) to initiate the reaction. After incubating 10 min at 25°C, GPb activity is assessed by measuring absorbance at 340 nm.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    After acclimation ob/ob and lean mice are randomized to the various treatment groups by body weight and fed glucose levels (tail snip) at 8 AM. Baseline plasma insulin samples are also taken from a subset of the animals representing each treatment group (n=10 ob/ob and n=10 lean ob/+ littermates). Two separate ob/ob and lean littermate studies are completed: 1) an initial 5 day study, and 2) a 14 day study to examine efficacy and more completely characterize the body weight change observed in the 5 day study. Treatment groups for the 5 day study are as follows: ob/ob vehicle (0.2% hydroxypropyl methylcellulose [HPMC], i.p., b.i.d.), A-592107 (10 or 100 mg/kg, i.p., b.i.d.), A-769662 (3 or 30 mg/kg, i.p., b.i.d.), AICAR (375 mg/kg, s.c., b.i.d.), or metformin (450 mg/kg, p.o., q.d., with vehicle in PM), and lean littermates treated with vehicle (i.p., b.i.d.). Treatment groups for the 14 day ob/ob and lean littermate study are as follows: ob/ob vehicle (0.2% HPMC, i.p., b.i.d.), A-769662 (3, 10, or 30 mg/kg, i.p., b.i.d.), or metformin, and lean littermates treated with vehicle or 30 mg/kg of A-769662 (i.p., b.i.d.).

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

    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 2.7748 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
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    A-769662 Related Classifications

    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 kinaseInhibitorinhibitorinhibit

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