AdipoRon

SKU: orb1223637

Description

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

Key Properties

• CAS Number: 924416-43-3
• MW: 428.52
• Purity: >98% (HPLC)
• Formula: C₂₇H₂₈N₂O₃
• SMILES: O=C(C1=CC=C(OCC(NC2CCN(CC3=CC=CC=C3)CC2)=O)C=C1)C4=CC=CC=C4
• Target: Adiponectin Receptor
• Solubility: Ethanol: 50 mg/mL (116.68 mM); DMSO: 86 mg/mL (200.69 mM)

Bioactivity

• In Vivo:
  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.
• In Vitro:
  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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

AdipoRon

Quick Database Links

Gene Symbol

Adiponectin Receptor