Amelparib

Amelparib (JPI-289 free base) is a potent, orally active, and water-soluble inhibitor of PARP-1. Amelparib inhibits PARP-1 activity (IC₅₀=18.5 nM) and cellular PAR formation (IC₅₀=10.7 nM) in the nanomolar range. Amelparib is a potential neuroprotective agent. Amelparib has the potential for the research of acute ischaemic stroke^[1]. IC50 & Target:IC50: 18.5 nM (PARP-1)^[1]. In Vitro:Amelparib (0.001 mM-1 mM; 2 h) dose-dependently reduces the number of apoptotic cells in cortical neurons induced by hypoxia for 24 h and 48 h^[1].
Amelparib (0, 0.01, 0.1 and 1 mM; 2 h) dose-dependently reduces the increased PARP activity in cortical neurons, the expression of cleaved caspase-3 in cortical neurons subjected to 6 h of hypoxia, and the levels of HIF-1α and PAR in cortical neurons subjected to 2 h of hypoxia^[1].
In Vivo:Amelparib (5, 7.5 and 10 mg/kg, i.v.; single dose) reduces infarct volume in rats with transient and permanent MCAO models by 30% and 53%, respectively, at a dose of 7.5 or 10 mg/kg^[2].
Amelparib (10 mg/kg, i.v.; single dose 2 or 8 h after MCAO) reduces mean infarct size and alleviates brain swelling in male SD rats^[2].
Amelparib (10 mg/kg, i.v.; single dose 2 h after MCAO) reduces apoptosis of penumbra cells in male SD rats^[2].