COH-SR4 是线粒体氧化磷酸化的解偶联剂，可调节 amp 依赖性激酶 (AMPK)-雷帕霉素 (mTOR) 信号的哺乳动物靶点，并抑制 hepg2 肝癌细胞的增殖。它对白血病、黑色素瘤、乳腺癌和肺癌显示出强大的抗增殖活性。它是一种AMPK活化剂，通过激活 AMPK 来抑制脂肪细胞分化，可用于肥胖及代谢紊乱相关的研究。

SR4 is a uncoupler of mitochondrial oxidative phosphorylation. SR4 modulating amp-dependent kinase (ampk)-mammalian target of rapamycin (mtor) signaling, and inhibiting proliferation of hepg2 hepatocarcinoma cells

SR4 is a novel mitochondrial uncoupler with anti-obesity and anti-diabetic properties.?SR4 increased oxygen consumption, dissipated mitochondrial membrane potential, induced mitochondrial swelling, and decreased intracellular ATP in cultured cells and isolated liver mitochondria.?Oral feeding of SR4 significantly reduced body weight gain, improved glycemic control and insulin resistance, and prevented dyslipidemia in both high-fat-diet (HFD) induced obese and diabetic db/db mice.?SR4 treatment also decreased liver triglycerides and prevented hepatic steatosis in both animal models.?Mitochondrial uncoupling of SR4 results to activation of AMP-activated protein kinase (AMPK), leading to the phosphorylation and inhibition of acetyl-CoA carboxylase (ACC).?Gene analyses by RT-PCR showed SR4 significantly suppressed the mRNA expression of several lipogenic genes and gluconeogenic genes in the liver of HFD obese mice.?RNA sequencing analysis showed that 642 genes were differentially expressed in liver of db/db mice after SR4 treatment (217 upregulated, 425 down-regulated).?Gene ontology analysis by DAVID indicated SR4 upregulated amino acid metabolism and down-regulated lipid and fatty acid synthesis and glucose metabolism.?These studies demonstrate that SR4 may be a promising compound for treatment of T2DM and obesity

73439-19-7

C13H8Cl4N2O

350.02

COH-SR4 (Mitochondria uncoupler SR4)

DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years