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Amelparib

Names

[ CAS No. ]:
1227156-72-0

[ Name ]:
Amelparib

[Synonym ]:
R252S84C2I
Benzo[h][1,6]naphthyridin-5(1H)-one, 10-ethoxy-2,3,4,6-tetrahydro-8-(4-morpholinylmethyl)-
Amelparib
10-Ethoxy-8-(4-morpholinylmethyl)-2,3,4,6-tetrahydrobenzo[h][1,6]naphthyridin-5(1H)-one

Biological Activity

[Description]:

Amelparib (JPI-289, JPI289) is a novel potent, water soluble PARP-1 inhibitor with IC50 of 18.5 nM, inhibits cellular PAR formation with IC50 of 10.7 nM; does not affect cell viability up to 1 mM in rat cortical neuronal cells; attenuates PARP activity restores ATP and NAD+ levels in oxygen glucose deprived (OGD) rat cortical neurons, reduces apoptosis-associated molecules such as apoptosis inducing factor (AIF), cytochrome C and cleaved caspase-3 in the OGD model; JPI-289 is a potential neuroprotective agent which could be useful as a treatment for acute ischaemic stroke. Stroke Phase 2 Clinical

[References]

References 1. Kim Y, et al. Clin Exp Pharmacol Physiol. 2017 Jun;44(6):671-679. 2. Kim Y, et al. Mol Neurobiol. 2018 Jan 30. doi: 10.1007/s12035-018-0910-6. View Related Products by Target PARP Stroke

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
569.6±50.0 °C at 760 mmHg

[ Molecular Formula ]:
C19H25N3O3

[ Molecular Weight ]:
343.420

[ Flash Point ]:
298.3±30.1 °C

[ Exact Mass ]:
343.189606

[ LogP ]:
1.04

[ Vapour Pressure ]:
0.0±1.6 mmHg at 25°C

[ Index of Refraction ]:
1.624

Related Compounds