Adiponectin Receptor

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

Arctiin (Arctigenin-4-glucoside) acts on an agonists of the adiponectin receptor 1 with anti-cancer effects.

Ticlopidine (PCR 5332) is an antiplatelet drug in the thienopyridine family which is an adenosine diphosphate (ADP) receptor inhibitor.

Gramine (Donaxine), a natural indole alkaloid, present in several plant species, acts as an active adiponectin receptor (AdipoR) agonist, with IC50s of 3.2 and 4.2 μM for AdipoR2 and AdipoR1, respectively. Gramine is also a human and mouse β2-Adrenergic receptor (β2-AR) agonist. Gramine has anti-tumor, anti-viral and anti-inflammatory properties.

Zeaxanthin dipalmitate (Physalien) is a lutein carotenoid found in fruits with anti-inflammatory, hepatoprotective, and anti-oxidative stress activity that attenuates ethanol-induced liver injury.Zeaxanthin dipalmitate restores mitochondrial autophagy, a function that has been inhibited by ethanol intoxication. Zeaxanthin dipalmitate protects degenerated photoreceptors in the retina of mice and improves visual acuity in a mouse model of photoreceptor degeneration, and may be used in studies of alcoholic fatty liver disease (AFLD) and retinitis pigmentosa (RP).

AdipoR agonist 1 (Compound 112254), acting as an agonist for the adiponectin receptor (AdipoR), stimulates transcriptional regulators including peroxisome proliferator-activated receptors (PPARs), peroxisome proliferator-activated receptor gamma coactivator 1α (PGC-1α), sirtuin 1 (SIRT1), and adenylate-activated protein kinase (AMPK). It is employed in the field of preventive doping research.

AdipoRon hydrochloride is a specific, orally active AdipoR agonist, capable of binding AdipoR1 (Kd: 1.8 μM) and AdipoR2 (Kd: 3.1 μM).