Uses
DR2313 is a potent, selective, competitive and brain-penetrant inhibitor of poly(ADP-ribose) polymerase (PARP), with IC50s of 0.20 μM and 0.24 μM for PARP-1 and PARP-2, respectively. DR2313 exhibits neuroprotective effects on ischemic injuries in vitro and in vivo[1][2].
Biological Activity
Potent, competitive inhibitor of poly(ADP-ribose) polymerase (PARP) (IC 50 values are 0.20 and 0.24 μ M for PARP-1 and PARP-2 respectively). Neuroprotective; reduces neuronal cell death in models of cerebral ischemia in vivo and in vitro . Brain penetrant.
References
[1] Nakajima H, et, al. A newly synthesized poly(ADP-ribose) polymerase inhibitor, DR2313 [2-methyl-3,5,7,8-tetrahydrothiopyrano[4,3-d]-pyrimidine-4-one]: pharmacological profiles, neuroprotective effects, and therapeutic time window in cerebral ischemia in rats. J Pharmacol Exp Ther. 2005 Feb;312(2):472-81. DOI:
10.1124/jpet.104.075465[2] Xu Z, et, al. Endonuclease G does not play an obligatory role in poly(ADP-ribose) polymerase-dependent cell death after transient focal cerebral ischemia. Am J Physiol Regul Integr Comp Physiol. 2010 Jul;299(1):R215-21. DOI:
10.1152/ajpregu.00747.2009
