1. Epigenetics PI3K/Akt/mTOR
  2. AMPK
  3. AMPK activator 4

AMPK activator 4 is a potent AMPK activator without inhibition of mitochondrial complex I. AMPK activator 4 selectively activates AMPK in the muscle tissues. AMPK activator 4 dose-dependently improves glucose tolerance in normal mice, and significantly lowers fasting blood glucose level and ameliorates insulin resistance in db/db diabetic mice. Anti-hyperglycemic effect.

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AMPK activator 4 Chemical Structure

AMPK activator 4 Chemical Structure

CAS No. : 2493239-46-4

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 275 In-stock
Solution
10 mM * 1 mL in DMSO USD 275 In-stock
Solid
5 mg USD 250 In-stock
10 mg USD 450 In-stock
25 mg USD 850 In-stock
50 mg USD 1350 In-stock
100 mg USD 1950 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

AMPK activator 4 is a potent AMPK activator without inhibition of mitochondrial complex I. AMPK activator 4 selectively activates AMPK in the muscle tissues. AMPK activator 4 dose-dependently improves glucose tolerance in normal mice, and significantly lowers fasting blood glucose level and ameliorates insulin resistance in db/db diabetic mice. Anti-hyperglycemic effect[1].

In Vitro

AMPK activator 4 (compound B10) (0-20 μM; 12-24 hours) induces phosphorylation of AMPK and its downstream protein ACC[1].
AMPK activator 4-mediated AMPK phosphorylation requires LKB1[1].
AMPK activator 4 slight decreases the viability of HepG2 cells after 72 hours of treatment at 10-20 μM[1].

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

Western Blot Analysis[1]

Cell Line: C2C12 myotubes, HepG2 and HuH-7 cells
Concentration: 0-20 μM
Incubation Time: 12-24 hours
Result: Induced dose-dependently phosphorylation of ACC in C2C12 myotube cells, and the phosphorylation of ACC was highly consistent with the phosphorylation of AMPK. Increased the phosphorylation of AMPK and ACC in human hepatocarcinoma HepG2 and HuH-7 cells.
In Vivo

AMPK activator 4 (100 mg/kg; Intragastrical administration; daily for 9 weeks) shows anti-hyperglycemic effect[1].

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

Animal Model: db/db mice (5-week old)[1]
Dosage: 100 mg/kg
Administration: Intragastrical administration; daily for 9 weeks
Result: Significantly lowered the fasting blood glucose in db/db mice (2-6 weeks). Significantly improved insulin resistance in db/db mice (for 9 weeks). The body weight and the serum levels of alanine aminotransferase (ALT) and aspartate aminotransferase (AST) (two markers of liver injury) were not significantly affected.
Molecular Weight

420.89

Formula

C24H21ClN2O3

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC(C)(OC1=CC=C(Cl)C=C1)C(NC2=CC=C(OCC3=CC=C(C#N)C=C3)C=C2)=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 : 250 mg/mL (593.98 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 2.3759 mL 11.8796 mL 23.7592 mL
5 mM 0.4752 mL 2.3759 mL 4.7518 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

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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    90% Corn Oil

    Solubility: ≥ 2.08 mg/mL (4.94 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

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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.
Purity & Documentation
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 2.3759 mL 11.8796 mL 23.7592 mL 59.3979 mL
5 mM 0.4752 mL 2.3759 mL 4.7518 mL 11.8796 mL
10 mM 0.2376 mL 1.1880 mL 2.3759 mL 5.9398 mL
15 mM 0.1584 mL 0.7920 mL 1.5839 mL 3.9599 mL
20 mM 0.1188 mL 0.5940 mL 1.1880 mL 2.9699 mL
25 mM 0.0950 mL 0.4752 mL 0.9504 mL 2.3759 mL
30 mM 0.0792 mL 0.3960 mL 0.7920 mL 1.9799 mL
40 mM 0.0594 mL 0.2970 mL 0.5940 mL 1.4849 mL
50 mM 0.0475 mL 0.2376 mL 0.4752 mL 1.1880 mL
60 mM 0.0396 mL 0.1980 mL 0.3960 mL 0.9900 mL
80 mM 0.0297 mL 0.1485 mL 0.2970 mL 0.7425 mL
100 mM 0.0238 mL 0.1188 mL 0.2376 mL 0.5940 mL
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AMPK activator 4 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.

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AMPK activator 4
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