Orally available NO-mimicking free radical trapping agent and sulfatase 2 (SULF2) inhibitor with in vivo efficacy in animal models of glioma and stroke.
Originally characterized for its NO-mimicking activity in preventing peroxynitrite formation and in vivo neuroprotective efficacy in animal models of cerebral ischemia (100 mg/kg i.v. in rabbits; 30-60 mg/kg plus 30-60 mg/kg/h i.v. or 50 mg/kg plus 8.8 mg/kg/h s.c. in rats; 28 mg/kg plus 16 mg/kg/h i.v. in monkeys), OKN-007 (HPN-07, NXY-059) is an orally available α-phenyl-tert-butylnitrone (PBN) derivative that is also shown to exhibit sulfatase 2 (SULF2) inhibitory activity and anticancer efficacy both in cultures (effective conc. 170-200 μM in Huh7 heptoma cultures) and in several rodent glioma models in vivo (C6, RG2, and GL261; 75 mg/kg/day for rats and 168 mg/kg/day for mice via drinking water).
NXY-059 is a novel nitrone with free radical-trapping properties that has a considerable neuroprotective effect in rats. We have now examined the efficacy of this drug at reducing long-term functional disability in a primate model of stroke. Twelve monkeys were
Free radicals have gained wide acceptance as mediators of cerebral ischemic injury. It has previously been reported that a spin trap nitrone, alpha-phenyl-N-tert-butyl nitrone (PBN), can reduce infarct volumes in rats subjected to either permanent or transient focal cerebral ischemia.
Journal of magnetic resonance imaging : JMRI, 31(4), 796-806 (2010-04-08)
To demonstrate that OKN007, a disulfonyl derivative of phenyl-tert-butyl nitrone (PBN), has anti-glioma activity in the clinically relevant C6 rat glioma model using multi-parametric magnetic resonance imaging. Twenty-one rats were intracerebrally implanted with C6 cells and administered OKN007 or kept
It has been proposed that the novel spin trap agent disodium-[(tert-butylimino)methyl]benzene-1,3-disulfonate N-oxide (NXY-059) may be useful in the treatment of ischemia and stroke. To date, there is little information concerning the safety of NXY-059 when administered in combination with the
Gliomas, the most common primary brain tumors in adults, have a poor outcome. PBN (α-phenyl-tert-butylnitrone) and OKN007 (2,4-disulfophenyl-PBN) are nitrones that have demonstrated beneficial effects in many aging diseases. In this study, we evaluated the anti-tumor effects of PBN and
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