PBT434

PBT434 is a potent, orally active and cross the blood-brain barrier α-synuclein aggregation inhibitor. PBT434 can be used as a iron chelator and modulates transcellular iron trafficking. PBT434 inhibits iron-mediated redox activity and iron-mediated aggregation of α-synuclein. PBT434 prevents the loss of substantia nigra pars compacta neurons (SNpc). PBT434 has the potential for the research of Parkinson’s disease (PD)^[1]. In Vitro: PBT434 (0-20 µM; 3 h) significantly inhibits H₂O₂ production by iron and significantly reduces the rate of Fe-mediated aggregation of α-synuclein^[1].
PBT434 (0-100 µM; 24 h) shows no cytotoxic effects on brain microvascular endothelial cells^[2].
PBT434 (20 µM; 24 h) incrases the expression of total TfR, Cp protein level in hBMVEC^[2]. In Vivo: PBT434 (30 mg/kg; p.o.; daily for 21 days) significantly preserved neuron numbers in the 6-OHDA intoxication model and shows significantly fewer rotations in the L-DOPA model, significantly reducing SNpc neuronal loss in the MPTP model^[1].