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Description

A cell-permeable, non-toxic naphthyl-oxazole compound that acts as a highly potent, selective, active site directed, mixed type inhibitor of lipoxygenase-12/15 (IC50 = 200 nM for human). The inhibition appears to be non-reductive and reversible in nature. Displays excellent selectivity over 5-LOX (IC50 >50 µ,M), 12-LOX (IC50 >100 µ,M), and 15-LOX (IC50 >100 µ,M) and does not affect the activity of COX-1 and -2 in any significant manner (<10% inhibition at 15 µ,M). Can cross the blood brain barrier (brain to plasma ratio = 2.8). Offers protection against glutamate-induced oxidative toxicity in mouse neuronal HT22 cells and reduces the size of infarcts in a murine model of ischemic stroke. Displays good aqueous stability over a wide range of pH. Exhibits attractive pharmacokinetic properties (t1/2 ~ 1 h in both plasma and brain, Cmax of 13.8 and 28.8 µ,M in plasma and brain, respectively, at 30 mg/kg, i.p)., A cell-permeable, non-toxic naphthyl-oxazole compound that acts as a highly potent, selective, active site directed, mixed type inhibitor of lipoxygenase-12/15 (IC50 = 200 nM for human). The inhibition appears to be non-reductive and reversible in nature. Displays excellent selectivity over 5-LOX (IC50 >50 µ,M), 12-LOX (IC50 >100 µ,M), and 15-LOX (IC50 >100 µ,M) and does not affect the activity of COX-1 and -2 in any significant manner (<10% inhibition at 15 µ,M). Can cross the blood brain barrier (brain to plasma ratio = 2.8). Offers protection against glutamate-induced oxidative toxicity in mouse neuronal HT22 cells and reduces the size of infarcts in a murine model of ischemic stroke. Displays good aqueous stability over a wide range of pH. Exhibits attractive pharmacokinetic properties (t1/2 ~ 1 h in both plasma and brain, Cmax of 13.8 and 28.8 µ,M in plasma and brain, respectively, at 30 mg/kg, i.p).Please note that the molecular weight for this compound is batch-specific due to variable water content.