AdipoRon (SC-396658) is an orally bioavailable adiponectin receptor agonist. It can combine with AdipoR1/2 (KD: 1.8/3.1 μM).

AdipoR1:1.8 μM(Kd), AdipoR2:3.1 μM(Kd)

在野生型小鼠体内,AdipoRon (50?mg/kg, p.o.)可激活肝脏中AdipoR2–PPAR-α通路,或者激活骨骼肌中AdipoR1–AMPK–PGC-1α通路,进而改善胰岛素耐受性,血脂异常及葡萄糖耐受性.在WT小鼠骨骼肌和肝脏中,AdipoRon (50?mg/kg, i.v.)通过AdipoR1/2使AMPK的磷酸化作用受到明显诱导.此外,AdipoRon可使遗传性肥胖啮齿类动物模型db/db小鼠的糖尿病症状得到改善,并使高脂饮食的db/db小鼠缩短的寿命延长.

通过与C2C12肌管中AdipoR1/2结合,AdipoRon可使AMPK活化作用增加,并促进PGC-1α表达以及线粒体生物合成。

The effects of AdipoRon on the proliferation of parenchymal and non-parenchymal hepatocytes are evaluated in vitro via L02 and RAW264.7, by MTT assay as described with slight modification: 100 μL cells suspension (6×104/mL) are seeded in a 96-well plate and incubated for 18 h. Fresh media with AdipoRon are added at specified concentrations, and the incubations continue for a further 24 h. Then cells are incubated for 4 h with 0.5 mg/mL of MTT, and analyzed in a microplate reader at 490 nm. Each group is performed in six replications. The mean absorbance values corrected for a blank (medium only) are calculated as percentages of survival.