1. Epigenetics PI3K/Akt/mTOR
  2. AMPK
  3. COH-SR4

COH-SR4 is an AMPK activator. COH-SR4 shows potent anti-proliferative activities against leukemia, melanoma, breast and lung cancers. COH-SR4 inhibits adipocyte differentiation via AMPK activation. COH-SR4 can be used for the research of obesity and related metabolic disorders.

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

COH-SR4 Chemical Structure

COH-SR4 Chemical Structure

CAS No. : 73439-19-7

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Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

  • References

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Description

COH-SR4 is an AMPK activator. COH-SR4 shows potent anti-proliferative activities against leukemia, melanoma, breast and lung cancers. COH-SR4 inhibits adipocyte differentiation via AMPK activation. COH-SR4 can be used for the research of obesity and related metabolic disorders[1].

IC50 & Target

AMPK[1]

In Vitro

COH-SR4 (1-5 μM; 24 hours) results in a dose-dependent increase in the phosphorylation of AMPK and its substrate ACC in 3T3-L1 preadipocytes, as well as in cancer cells such as HL-60, HeLa, MCF-7[1].
COH-SR4 (3-5 µM; 7 days) significantly inhibits 3T3-L1 adipocyte differentiation in a dose-dependent manner[1].
COH-SR4 (1-5 μM; 24 hours) promotes cell G1 cycle arrest[1].
COH-SR4 significantly reduces intracellular lipid accumulation and downregulates the expression of key adipogenesis-related transcription factors and lipogenic proteins[1].

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

Western Blot Analysis[1]

Cell Line: 3T3-L1 preadipocytes, HL-60 cells, HeLa cells, MCF-7 cells
Concentration: 1 μM, 3 μM, 5 μM
Incubation Time: 24 hours
Result: Indirectly activated AMPK.

Cell Cycle Analysis[1]

Cell Line: 3T3-L1 cells
Concentration: 1 μM, 3 μM, 5 μM
Incubation Time: 24 hours
Result: Modulated the level of proteins active during S and G2 phases of the cell cycle.
In Vivo

COH-SR4 (5 mg/kg; i.g.; 3x/week; for 6 weeks) reduces body weight and fat mass in high fat diet (HFD) obese mice without affecting food intake[2].
COH-SR4 improves glycemic control and dyslipidemia in HFD obese mice[2].
COH-SR4 decreases adipose tissue hypertrophy and affects circulating adipokine levels in HFD obese mice[2].
COH-SR4 prevents hepatic lipid accumulation and fatty liver in HFD obese mice[2].

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

Animal Model: Nine-week old male C57BL/6J mice[2]
Dosage: 5 mg/kg
Administration: Oral gavage, three times a week, for 6 weeks
Result: Decreased body weight and fat mass in HFD obese mice.
Molecular Weight

350.03

Formula

C13H8Cl4N2O

CAS No.
Appearance

Solid

Color

Gray to gray purple

SMILES

O=C(NC1=CC(Cl)=CC(Cl)=C1)NC2=CC(Cl)=CC(Cl)=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (357.11 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 2.8569 mL 14.2845 mL 28.5690 mL
5 mM 0.5714 mL 2.8569 mL 5.7138 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

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: 2.08 mg/mL (5.94 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    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% Corn Oil

    Solubility: ≥ 2.08 mg/mL (5.94 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:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

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: 99.45%

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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8569 mL 14.2845 mL 28.5690 mL 71.4224 mL
5 mM 0.5714 mL 2.8569 mL 5.7138 mL 14.2845 mL
10 mM 0.2857 mL 1.4284 mL 2.8569 mL 7.1422 mL
15 mM 0.1905 mL 0.9523 mL 1.9046 mL 4.7615 mL
20 mM 0.1428 mL 0.7142 mL 1.4284 mL 3.5711 mL
25 mM 0.1143 mL 0.5714 mL 1.1428 mL 2.8569 mL
30 mM 0.0952 mL 0.4761 mL 0.9523 mL 2.3807 mL
40 mM 0.0714 mL 0.3571 mL 0.7142 mL 1.7856 mL
50 mM 0.0571 mL 0.2857 mL 0.5714 mL 1.4284 mL
60 mM 0.0476 mL 0.2381 mL 0.4761 mL 1.1904 mL
80 mM 0.0357 mL 0.1786 mL 0.3571 mL 0.8928 mL
100 mM 0.0286 mL 0.1428 mL 0.2857 mL 0.7142 mL
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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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COH-SR4
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