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.
IC50&Target
AMPK
体外研究
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.
COH-SR4 (3-5 µM; 7 days) significantly inhibits 3T3-L1 adipocyte differentiation in a dose-dependent manner.
COH-SR4 (1-5 μM; 24 hours) promotes cell G1 cycle arrest.
COH-SR4 significantly reduces intracellular lipid accumulation and downregulates the expression of key adipogenesis-related transcription factors and lipogenic proteins.
Western Blot Analysis
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
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.
体内研究
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.
COH-SR4 improves glycemic control and dyslipidemia in HFD obese mice.
COH-SR4 decreases adipose tissue hypertrophy and affects circulating adipokine levels in HFD obese mice.
COH-SR4 prevents hepatic lipid accumulation and fatty liver in HFD obese mice.
Animal Model:
Nine-week old male C57BL/6J mice
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.
分子式
C13H8N2OCl4
分子量
350.03
CAS号
73439-19-7
运输条件
Room temperature in continental US; may vary elsewhere.