| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
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| 100mg |
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| Other Sizes |
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| Targets |
AMPK[1]
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|---|---|
| ln Vitro |
In 3T3-L1 preadipocytes and cancer cells like HL-60, HeLa, and MCF-7, COH-SR4 (1–5 μM; 24 hours) causes a dose-dependent increase in the phosphorylation of AMPK and its substrate ACC[1]. Significant inhibition of 3T3-L1 adipocyte differentiation is observed in a dose-dependent manner with COH-SR4 (3-5 μM; 7 days)[1]. In a 24-hour period, COH-SR4 (1–5 μM) stimulates cell G1 cycle arrest[1]. Key transcription factors associated with adipogenesis and lipogenic proteins are downregulated when COH-SR4 is present, leading to a significant reduction in intracellular lipid accumulation[1].
|
| ln Vivo |
In obese mice fed a high-fat diet (HFD), COH-SR4 (5 mg/kg; ig; three times/week; for six weeks) decreases body weight and fat mass without changing food intake[2]. In HFD obese mice, COH-SR4 improves dyslipidemia and glycemic control[2]. In HFD obese mice, COH-SR4 reduces adipose tissue hypertrophy and modifies circulating adipokine levels[2]. In HFD obese mice, COH-SR4 prevents hepatic lipid accumulation and fatty liver[2].
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: 3T3-L1 preadipocytes, HL-60 cells, HeLa cells, MCF-7 cells Tested Concentrations: 1 μM, 3 μM, 5 μM Incubation Duration: 24 hrs (hours) Experimental Results: Indirectly activated AMPK. Cell Cycle Analysis[1] Cell Types: 3T3-L1 cells Tested Concentrations: 1 μM, 3 μM, 5 μM Incubation Duration: 24 hrs (hours) Experimental Results: Modulated the level of proteins active during S and G2 phases of the cell cycle. |
| Animal Protocol |
Animal/Disease Models: Nine-week old male C57BL/6J mice[2]
Doses: 5 mg/kg Route of Administration: po (oral gavage), three times a week, for 6 weeks Experimental Results: diminished body weight and fat mass in HFD obese mice. |
| References |
[1]. James L Figarola, et al. Small‑molecule COH-SR4 inhibits adipocyte differentiation via AMPK activation. Int J Mol Med. 2013 May;31(5):1166-76.
[2]. James Lester Figarola, et al. COH-SR4 Reduces Body Weight, Improves Glycemic Control and Prevents Hepatic Steatosis in High Fat Diet-Induced Obese Mice. PLoS One. 2013; 8(12): e83801. |
| Molecular Formula |
C13H8CL4N2O
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|---|---|
| Molecular Weight |
350.03
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| CAS # |
73439-19-7
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| SMILES |
ClC1C=C(Cl)C=C(NC(NC2=CC(Cl)=CC(Cl)=C2)=O)C=1
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : 125 mg/mL (357.11 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.08 mg/mL (5.94 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.94 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.2857 mL | 1.4284 mL | 2.8569 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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