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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-PARP-Amelparib hydrochloric hydrate
Amelparib hydrochloric hydrate

Chemical Structure : Amelparib hydrochloric hydrate

CAS No.: 1449233-60-6

Amelparib hydrochloric hydrate (JPI-289;JPI289)

货号: PC-35442Not For Human Use, Lab Use Only.

Amelparib hydrochloric hydrate (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.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

Amelparib hydrochloric hydrate (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

物理化学性质&存储条件

分子量 452.373
分子式 C19H31Cl2N3O5
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

10-ethoxy-8-(morpholinomethyl)-2,3,4,6-tetrahydrobenzo[h][1,6]naphthyridin-5(1H)-one dihydrochloride dihydrate

参考文献

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.

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