AdipoRon

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

AdipoRon 是一种新型口服生物可用脂联素受体激动剂，AdipoR1 和 AdipoR2 的 KD 分别为 1.8 和 3.1 μM。

AdipoRon is a novel, and orally bioavailable adiponectin receptor agonist with KD of 1.8 and 3.1 μM for AdipoR1 and AdipoR2, respectively.

AdipoRon is an orally active and specific AdipoR agonist, binds to AdipoR1 and AdipoR2, with Kds of 1.8 and 3.1 μM. AdipoRon (50 nM-50 μM) increases AMPK phosphorylation via AdipoR1. AdipoRon (50 μM) dose-dependently attenuates the expression of TNF-α and TGF-β1 in the L02 cells. AdipoRon exhibits significant and dosage-dependent growth suppression on macrophages. AdipoRon treatment significantly improves cardiac functional recovery after reperfusion, and inhibits post-MI apoptosis. AdipoRon exerts vasodilation by mechanisms distinct to adiponectin and induces vasorelaxation without a marked decrease in VSMC [Ca2+]i.

AdipoRon (50?mg/kg, i.v.) cuases significant phosphorylation of AMPK in skeletal muscle and liver of wild-type mice but not Adipor1?/??Adipor2?/? double-knockout mice. AdipoRon (0.02, 0.1, and 0.5 mg/kg, i.g.) alleviates D-GalN induced hepatotoxicity in mice, and prevents hepatic architecture distortion against D-GalN challenge. The hepatoprotective potential of AdipoRon is particularly evident in higher dosages (0.1 and 0.5 mg/kg). Enhanced cardiomyocyte apoptosis in APN-deficient mice is rescued by AdipoRon (50 mg/kg, p.o.) administration. Antiapoptotic effect of AdipoRon is attenuated but not lost in AMPK-DN mice.

AdipoRon

Neuroscience

Adiponectin Receptor

AdipoR1| AdipoR2

Metabolic Disease

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924416-43-3

428.52

C27H28N2O3

>98% (HPLC)

Ethanol: 50 mg/mL (116.68 mM); DMSO: 86 mg/mL (200.69 mM)

O=C(C1=CC=C(OCC(NC2CCN(CC3=CC=CC=C3)CC2)=O)C=C1)C4=CC=CC=C4

2-(4-benzoylphenoxy)-N-(1-benzylpiperidin-4-yl)acetamide

(-20℃)

With Ice Pack

≥ 2 years