2-Methyl-3,5,7,8-tetrahydrothiopyrano[4,3-d]pyrimidine-4-one White solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. A brain-permeable and water soluble pyrimidinone compound that acts as a potent and NAD+-competitive inhibitor of PARP (IC50 = 200 nM and 240 nM for rhPARP1 and rmPARP2, respectively) with little activity against the dehydrogenase activity of GAPDH, ADH, LDH, or the ADP-ribosylase activity of bacterial diphtheria toxin even at concentrations as high as 10 µM. Shown to inhibit H2O2-induced PAR formation and neuronal cell death in primary rat cerebral cortex culture in vitro (EC50 = 270 nM) and exhibit neuroprotective effects in both permanent and transient focal ischemia models in rat in in vivo. Purity: ≥98% by HPLC. CAS 284028-90-6. Ref.: Nakajima, H., et al. 2005. J. Pharmacol. Exp. Ther. 312, 472. |
