AMPK activator 10

AMPK activator 10 is an orally active, potent AMPK activator with EC150 of 44.3 nM by cell-ELISA. AMPK activator 10 increases the phosphorylation levels of ACC. AMPK activator 10 exhibits a glucose lowering effect[1].

Signaling Pathways >> Epigenetics >> AMPK

Signaling Pathways >> PI3K/Akt/mTOR >> AMPK

Research Areas >> Metabolic Disease

AMPK

AMPK activator 10 (化合物14d; 0.3, 1, 3 mg/kg; 口服灌胃; 一天2次; 21 天) 表现出降糖作用[1]。 AMPK activator 10 (0.06, 0.19, 0.56, 1.67, 5 mg/kg; 口服灌胃; 单剂量) 以剂量依赖性方式导致 ACC 的磷酸化水平升高，ACC 是 AMPK 的下游靶分子 [1]。 AMPK activator 10 (0.5 mg/kg 静脉注射或 1.0 mg/kg 口服灌胃) 在大鼠中的 CL 为 9.02 mL/min•kg，Cmax 为 65.4 ng/mL，AUC 为 347 ng •h/mL[1]。 Animal Model: KKAy mice[1] Dosage: 0.3, 1, 3 mg/kg Administration: Orally; bid; for 21 days Result: Exhibited a glucose lowering effect. The increase in hemoglobin A1c (ΔHbA1c) between day 0 and day 21 was dose-dependently suppressed in the 14d dosed group. Animal Model: Rats[1] Dosage: 0.5 mg/kg by iv or 1.0 mg/kg by po Administration: IV or po Result: Had a CL of 9.02 mL/min•kg, a Cmax of 65.4 ng/mL and an AUC of 347 ng•h/mL.

[1]. Yuusuke Tamura, et al. Identification of novel benzimidazole derivatives as highly potent AMPK activators with anti-diabetic profiles. Bioorg Med Chem Lett. 2023 Jan 1;79:129059.