Molecular Formula | C17H17N3O2HCl
|
Molar Mass | 331.8 |
Solubility | H2O: soluble22mg/mL |
Appearance | White solid |
Color | white to yellow |
Storage Condition | Keep in dark place,Inert atmosphere,Store in freezer, under -20°C |
Stability | Stable for 2 years from date of purchase as supplied. Solutions in DMSO or distilled water may be stored at -20° for up to 3 months. |
Sensitive | Light Sensitive & Hygroscopic |
Use | PJ34 HCl is a hydrochloride form of PJ34 and is a PARP inhibitor with EC50 of 20 nM, which is equally effective on PARP1/2. |
In vitro study | PJ34 inhibits the PARP enzyme activity with an IC 50 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. |
In vivo study | 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. |