AMPK activator 4

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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.

AMPK activator 4 (compound B10) (0-20 μM; 12-24 hours) induces phosphorylation of AMPK and its downstream protein ACC.AMPK activator 4-mediated AMPK phosphorylation requires LKB1. AMPK activator 4 slight decreases the viability of HepG2 cells after 72 hours of treatment at 10-20 μM.Western Blot Analysis Cell Line:C2C12 myotubes, HepG2 and HuH-7 cells Concentration:0-20 μM Incubation Time:12-24 hours Result: Induced dose-dependently phosphorylation of ACC in C2C12 myotube cells, and the phosphorylation of ACC was highly consistent with the phosphorylation of AMPK. Increased the phosphorylation of AMPK and ACC in human hepatocarcinoma HepG2 and HuH-7 cells.

AMPK activator 4 (100 mg/kg; Intragastrical administration; daily for 9 weeks) shows anti-hyperglycemic effect.Animal Model:db/db mice (5-week old) Dosage:100 mg/kg Administration:Intragastrical administration; daily for 9 weeks Result:Significantly lowered the fasting blood glucose in db/db mice (2-6 weeks). Significantly improved insulin resistance in db/db mice (for 9 weeks). The body weight and the serum levels of alanine aminotransferase (ALT) and aspartate aminotransferase (AST) (two markers of liver injury) were not significantly affected.

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Membrane Transporter/Ion Channel

AMPK

AMPK

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2493239-46-4

420.89

C24H21ClN2O3

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 250 mg/mL (593.98 mM; 超声助溶 )

CC(C)(Oc1ccc(Cl)cc1)C(=O)Nc1ccc(OCc2ccc(cc2)C#N)cc1

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(-20℃)

With Ice Pack

≥ 2 years