ZLN024 是有效的AMPK变构激活剂，直接激活重组 AMPK α1β1γ1，AMPK α2β1γ1，AMPK α1β2γ1 和 AMPK α2β2γ1 异源三聚体，EC50分别为 0.42 μM，0.95 μM，1.1 μM 和 0.13 μM。

ZLN024 is an activator of AMPK allosteric. ZLN024 allosterically stimulates active AMPK heterotrimers and the inactive α1 subunit truncations α1 (1-394) and α1 (1-335) but not α1 (1-312).

ZLN024 allosterically stimulates active AMPK heterotrimers and the inactive α1 subunit truncations α1 (1-394) and α1 (1-335) but not α1 (1-312). ZLN024 increases the activity of α1β1γ1 by 1.5-fold and has an EC50 of 0.42 μM, and it increases the activity of α2β1γ1 by 1.7-fold with an EC50 of 0.95 μM. ZLN024 also directly activates recombinant AMPK α1β2γ1, by 1.7-fold with an EC50 of 1.1 μM; and AMPK α2β2γ1, by 1.6-fold with an EC50 of 0.13 μM.

C57BKS db/db mice are administered a 15 mg/kg/day dose of ZLN024 by daily gavage for 5 weeks; 250 mg/kg/day Metformin (Met) is used as a positive control. After 4 weeks of treatment, ZLN024 improves glucose tolerance. ZLN024 reduces the fasting blood glucose by 15%. Liver tissue weight, triacylglycerol and the total cholesterol content are decreased.

723249-01-2

C13H13BrN2OS

325.22

DMSO:50 mg/ml (153.74 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years