2095489-35-1

BRF110 is a brain penetrant, potent and selective agonist of nuclear receptor-related 1 (Nurr1):Retinoid X receptor α (RXRα) heterodimer. BRF110 is a neuroprotective agent that prevents dopaminergic neuron demise and striatal dopaminergic denervation in vivo against PD-causing toxins. It induced dopamine biosynthesis in vivo. BRF110 chronic dosing does not induce dyskinesia in mice model.

BRF110 is the selective, orally active rexinoid for Nurr1-RXRα, that selectively activates the Nurr1-RXRα heterodimer with an EC50 of 0.9 μM in SH-SY5Y. BRF110 upregulates the expression of BDNF, exhibits neuroprotective activity against MPP+ induced toxicity. BRF110 can cross blood-brain barrier[1].

[1] Asvos X, et al., BRF110, an Orally Active Nurr1-RXRα-Selective Rexinoid, Enhances BDNF Expression without Elevating Triglycerides. J Med Chem. 2025 Feb 27;68(4):4763-4786. DOI:10.1021/acs.jmedchem.4c03046