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PJ34 hydrochloride

SKU: orb1225243

Description

PJ34 hydrochloride is the hydrochloride salt of PJ34, which is a PARP inhibitor with EC50 of 20 nM and is equally potent to PARP1/2.

Images & Validation

Key Properties

CAS Number344458-15-7
MW311.8
Purity>98% (HPLC)
FormulaC17H18ClN3O2
SMILESCN(C)C(=O)CC1=CC2=C(NC(=O)C3=CC=CC=C23)C=C1
TargetPARP
SolubilityWater: 66 mg/mL (198.91 mM); DMSO: 66 mg/mL (198.91 mM)

Bioactivity

In Vivo
To compare the potency and efficacy with other PARP inhibitors, PJ34 is evaluated at the doses of 3.2 and 10 mg/kg, respectively. PJ34 at the dose of 3.2 mg/kg significantly reduces cortical damage by 33%; however, 10 mg/kg dosing shows reversed effect (17% reduction). PJ34 (25 mg/kg) reduces the levels of TNF-α mRNA in ischemic animals by 70% and these values in treated mice do not differ from that of sham or naive animals. Treatment of ischemic mice with PJ34 reduces the level of E-selectin mRNA by 81% and that of ICAM-1 mRNA by 54%, compared to vehicle-treated ischemic mice.
In Vitro
PJ34 inhibits the PARP enzyme activity with an IC50 of 110±1.9 nM. To compare the neuroprotective properties of other PARP inhibitors in PC12 cells, PJ34 is evaluated using by LDH assay. PJ34 treatment also significantly and concentration dependently attenuates cell death at a concentration ranging from 10-7 to 10-5 M.

Storage & Handling

StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

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Protocol Information

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500 mg
10 mg
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100 mg
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