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Chemical Structure| 73439-19-7 Chemical Structure| 73439-19-7

Structure of COH-SR4
CAS No.: 73439-19-7

Chemical Structure| 73439-19-7

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COH-SR4 is an AMPK activator with anticancer properties. It significantly inhibited adipocyte differentiation in a dose-dependent manner in 3T3-L1 cells. It significantly reduced intracellular lipid accumulation and downregulated the expression of key adipogenesis-related transcription factors and lipogenic proteins in differentiating adipocytes.

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Product Details of COH-SR4

CAS No. :73439-19-7
Formula : C13H8Cl4N2O
M.W : 350.03
SMILES Code : O=C(NC1=CC(Cl)=CC(Cl)=C1)NC2=CC(Cl)=CC(Cl)=C2
MDL No. :MFCD01566238
InChI Key :VKVJIWVUYNTBEZ-UHFFFAOYSA-N
Pubchem ID :595311

Safety of COH-SR4

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P280-P301+P312-P302+P352-P305+P351+P338

Related Pathways of COH-SR4

epigenetics
PI3K-AKT

Isoform Comparison

Biological Activity

Description
COH-SR4 activates AMPK and exhibits strong anti-proliferative effects against leukemia, melanoma, breast, and lung cancers. It hinders adipocyte differentiation by activating AMPK. COH-SR4 is a valuable tool for studying obesity and associated metabolic disorders[1].

In Vitro:

Cell Line
Concentration Treated Time Description References
A549 cells 1, 3, 5, 10 μM 4 h SR4 activated phosphorylation of AMPK and ACC in LKB1-deficient A549 cells, indicating its AMPK activation is independent of LKB1 and CaMKKβ. PLoS One. 2013 Dec 20;8(12):e83801
HepG2 cells 1, 3, 5, 10 μM 4 h SR4 increased phosphorylation of AMPK and ACC in a concentration-dependent manner, similar to the AMPK activator AICAR. PLoS One. 2013 Dec 20;8(12):e83801
HAVSMC cells 0–200 μM 96 h To evaluate the effect of SR4 on the survival of HAVSMC cells, results showed SR4 did not cause significant cytotoxicity. Biochem Pharmacol. 2012 Dec 1;84(11):1419-27
A2058 cells 11 ± 2 μM (IC50) 96 h To evaluate the effect of SR4 on the survival of A2058 cells, results showed SR4 significantly inhibited cell survival. Biochem Pharmacol. 2012 Dec 1;84(11):1419-27
Hs600T cells 6 ± 1 μM (IC50) 96 h To evaluate the effect of SR4 on the survival of Hs600T cells, results showed SR4 significantly inhibited cell survival. Biochem Pharmacol. 2012 Dec 1;84(11):1419-27
B16-F0 cells 5 ± 1 μM (IC50) 96 h To evaluate the effect of SR4 on the survival of B16-F0 cells, results showed SR4 significantly inhibited cell survival. Biochem Pharmacol. 2012 Dec 1;84(11):1419-27

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6J mice High-fat diet-induced obese mice Oral 5 mg/kg Three times a week for 6 weeks SR4 significantly reduced body weight and fat mass in HFD-induced obese mice, improved glycemic control and insulin sensitivity, lowered plasma lipid levels, prevented hepatic steatosis, and increased AMPK activation in liver and adipose tissues. PLoS One. 2013 Dec 20;8(12):e83801
C57B mice and Hsd: Athymic nude nu/nu mice B16-F0 mouse melanoma model and A2058 human melanoma mouse xenograft model Oral gavage 4 mg/kg Alternate day administration for 8 weeks To evaluate the anti-tumor effect of SR4 in vivo, results showed SR4 significantly inhibited tumor burden and was well tolerated. Biochem Pharmacol. 2012 Dec 1;84(11):1419-27

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.86mL

0.57mL

0.29mL

14.28mL

2.86mL

1.43mL

28.57mL

5.71mL

2.86mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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