| Identification | Back Directory | [Name]
Amelparib | [CAS]
1227156-72-0 | [Synonyms]
Amelparib
Benzo[h]-1,6-naphthyridin-5(1H)-one, 10-ethoxy-2,3,4,6-tetrahydro-8-(4-morpholinylmethyl)- | [Molecular Formula]
C19H25N3O3 | [MOL File]
1227156-72-0.mol | [Molecular Weight]
343.42 |
| Hazard Information | Back Directory | [Uses]
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]. | [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].
| Animal Model: | Male Sprague–Dawley rats[2] | | Dosage: | 10 mg/kg | | Administration: | Intravenous injection (i.v.), 2 h after MCAO | | Result: | Reduced the infarct area by 53% and the number of apoptotic cells by 56% after 24 h of administration. |
| [References]
[1] Kim Y, et al. Neuroprotective effects of a novel poly (ADP-ribose) polymerase-1 inhibitor, JPI-289, in hypoxic rat cortical neurons. Clin Exp Pharmacol Physiol. 2017;44(6):671-679. DOI:10.1111/1440-1681.12757
[2] Youngchul Kim, et al. Early treatment with poly (ADP-ribose) polymerase-1 inhibitor (JPI-289) reduces infarct volume and improves long-term behavior in an animal model of ischemic stroke. Molecular neurobiology 55 (2018): 7153-7163. DOI:10.1007/s12035-018-0910-6 |
|
|