| 产品描述： | PJ34 hydrochloride is an inhibitor of PARP1/2 with IC50 of 110 nM and 86 nM, respectively. |
| 靶点： |
PARP:110 nM (IC50);PARP-2:86 nM (IC50);PARP-1:110 nM (IC50);PARP |
| 体内研究： |
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 |
| 参考文献： |
1. Iwashita A, et al. A novel and potent poly(ADP-ribose) polymerase-1 inhibitor, FR247304 (5-chloro-2-[3-(4-phenyl-3,6-dihydro-1(2H)-pyridinyl)propyl]-4(3H)-quinazolinone), attenuates neuronal damage in in vitro and in vivo models of cerebral ischemia. J Ph 2. Haddad M, et al. Anti-inflammatory effects of PJ34, a poly(ADP-ribose) polymerase inhibitor, in transient focal cerebral ischemia in mice. Br J Pharmacol. 2006 Sep;149(1):23-30. 3. Diani-Moore S, et al. NAD+ loss, a new player in AhR biology: prevention of thymus atrophy and hepatosteatosis by NAD+ repletion. Sci Rep. 2017 May 23;7(1):2268. |
| 溶解性： |
DMSO : 12.5 mg/mL (37.67 mM; ultrasonic and warming and heat to 60°C) |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
3.014 ml |
15.069 ml |
30.139 ml |
| 5 mM |
0.603 ml |
3.014 ml |
6.028 ml |
| 10 mM |
0.301 ml |
1.507 ml |
3.014 ml |
| 50 mM |
0.06 ml |
0.301 ml |
0.603 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京