UPF 1069 is a selective PARP2 inhibitor with IC50 of 0.3 μM. UPF 1069 inhibits PARP1 with IC50 of 8 μM. In mouse mixed cortical cells exposed to OGD, UPF-1069 (1-10 mM) significantly reduces post-ischaemic damage. UPF 1069 (0.1-1 µM) markedly enhances CA1 hippocampal damage. UPF 1069 (10 µM) also exacerbates oxygen-glucose deprivation (OGD) damage in organotypic hippocampal slices.
|Animal models||Rats deprived of hippocampi.|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 55 mg/mL|
Selective PARP-2 inhibitors increase apoptosis in hippocampal slices but protect cortical cells in models of post-ischaemic brain damage.
Moroni F, et al. Br J Pharmacol. 2009 Jul;157(5):854-62. PMID: 19422384.
|Related PARP Products|
Benzamide is an inhibitor of poly(ADP-ribose) polymerase with an IC50 of 3.3 μM.
Picolinamide is a strong inhibitor of poly (ADP-ribose) synthetase of nuclei from rat pancreatic islet cells.
|Niraparib (MK-4827) tosylate
Niraparib (MK-4827) tosylate is an excellent PARP1 and PARP2 inhibitor with IC50 of 3.8 and 2.1 nM, respectively.
Daidzein is an inactive analogue of genistein, a tyrosine kinase inhibitor and an estrogen receptor activator.
NMS-P118 is a potent, orally available, and highly selective PARP-1 inhibitor endowed with excellent ADME and pharmacokinetic profiles, showing 150-fold selectivity for PARP-1 over PARP-2 (Kd 0.009 μM vs 1.39 μM, respectively).
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.