S80661 |
PJ34 HCl |
源叶(MedMol) | 97% |
- 提示:详情请下载说明书。
- 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
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)