AdipoRon

SKU: orb1305879

Description

AdipoRon (SC-396658) is an orally active small molecule agonist for the AdipoR1 and AdipoR2 receptors, with binding affinities (K_D) of 1.8 µM and 3.1 µM, respectively. It is widely used in research to study metabolic diseases, including type 2 diabetes and obesity, in both cellular and animal models.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 924416-43-3
• MW: 428.52
• Purity: 99.63%
• Formula: C₂₇H₂₈N₂O₃
• SMILES: O=C(COc1ccc(cc1)C(=O)c1ccccc1)NC1CCN(Cc2ccccc2)CC1
• Target: Adiponectin Receptor
• Solubility: H2O:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (9.33 mM);Ethanol:50 mg/mL (116.68 mM);DMSO:100 mg/mL (233.36 mM)

Bioactivity

• Target IC50:
  AdipoR2:3.1 μM(Kd)|AdipoR1:1.8 μM(Kd)
• In Vivo:
  AdipoRon, through its interaction with AdipoR1/2 in C2C12 myotubes, enhances the activation of AMPK and promotes the expression of PGC-1α as well as mitochondrial biogenesis.
• In Vitro:
  In wild-type mice, AdipoRon administered orally (50 mg/kg) activates the AdipoR2–PPAR-α pathway in the liver or the AdipoR1–AMPK–PGC-1α pathway in skeletal muscle, thereby improving insulin resistance, lipid abnormalities, and glucose tolerance. In the skeletal muscle and liver of WT mice, AdipoRon (50 mg/kg, intravenously) significantly induces phosphorylation of AMPK via AdipoR1/2. Furthermore, AdipoRon ameliorates diabetic symptoms in the genetic obesity murine model db/db mice and extends the shortened lifespan of db/db mice on a high-fat diet.
• Cell Research:
  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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

SC 396658, SC396658, SC-396658, Adiponectin Receptor, Adiponectin receptor, AdipoR2, AdipoRon, AdipoRs, AdipoR1, Adiponectinreceptor, inhibit, Inhibitor

Compound Identifiers

PubChem CID

16307093