AMPK activator 4 是一种有效 AMPK 激活剂，并且不抑制线粒体复合物 I。AMPK activator 4 选择性地激活肌肉组织中的 AMPK。AMPK activator 4 剂量依赖性地改善正常小鼠的糖耐量，显著降低 db/db 糖尿病小鼠的空腹血糖水平和改善胰岛素抵抗。具有降血糖作用。
AMPK activator 4 is a potent AMPK activator without inhibition of mitochondrial complex I. AMPK activator 4 selectively activates AMPK in the muscle tissues. AMPK activator 4 dose-dependently improves glucose tolerance in normal mice, and significantly lowers fasting blood glucose level and ameliorates insulin resistance in db/db diabetic mice. Anti-hyperglycemic effect[1].
AMPK activator 4 (compound B10) (0-20 μM; 12-24 hours) induces phosphorylation of AMPK and its downstream protein ACC[1].AMPK activator 4-mediated AMPK phosphorylation requires LKB1[1].AMPK activator 4 slight decreases the viability of HepG2 cells after 72 hours of treatment at 10-20 μM[1].
AMPK activator 4 (100 mg/kg; Intragastrical administration; daily for 9 weeks) shows anti-hyperglycemic effect[1].
[1]. Sun G, You Y, Li H, et al. Discovery of AdipoRon analogues as novel AMPK activators without inhibiting mitochondrial complex I. Eur J Med Chem. 2020;200:112466.
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