IC50: 23 nM (ACC2)[2]
A-908292 is a potent and selective acetyl-CoA carboxylase 2 (ACC2) inhibitor, with an IC50 of 23 nM for human ACC2. A-908292 can be used for the research of fatty acid metabolism[1][2].
A-908292 (30 mg/kg; p.o.; twice a day for 2 weeks) 可降低 ob/ob 小鼠的血清葡萄糖和甘油三酯水平[2]。
A-908292 (15 mg/kg; p.o.; twice a day for 4 days) 可显着降低 ACC2 敲除小鼠的血浆甘油三酯水平[3]。
A-908292 (30-100 mg/kg; p.o.; twice a day for 3 days) 可刺激大鼠体内的 PPAR-α 依赖性信号传导通路[2]。
[1]. Nishiura Y, et, al. Discovery of a novel olefin derivative as a highly potent and selective acetyl-CoA carboxylase 2 inhibitor with in vivo efficacy. Bioorg Med Chem Lett. 2018 Aug 1;28(14):2498-2503.
[2]. Waring JF, et, al. Gene expression analysis in rats treated with experimental acetyl-coenzyme A carboxylase inhibitors suggests interactions with the peroxisome proliferator-activated receptor alpha pathway. J Pharmacol Exp Ther. 2008 Feb;324(2):507-16.
[3]. Takagi H, et, al. A Novel Acetyl-CoA Carboxylase 2 Selective Inhibitor Improves Whole-Body Insulin Resistance and perglycemia in Diabetic Mice through Target-Dependent Pathways. J Pharmacol Exp Ther. 2020 Mar;372(3):256-263.