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ML351 is a potent and selective inhibitor of human 15-lipoxygenase-1 with IC50 value of 200 nM [1][2].

Human lipoxygenases (LOX) are nonheme iron-containing enzymes that catalyze the dioxygenation of polyunsaturated fatty acids (e.g., linoleic acid (LA) and arachidonic acid (AA)) to form hydroperoxy fatty acids [1][2]. Human reticulocyte 15-lipoxygenase-1 is an attractive therapeutic target for its role in atherogenesis, diabetes, Alzheimer’s disease, new-born periventricular leukomalacia, breast cancer, and stroke [2].

ML351 is a potent and selective 15-lipoxygenase inhibitor. ML351 exhibited nanomolar potency and excellent selectivity (>250-fold) versus 5-LOX, platelet 12-LOX, 15-LOX-2, ovine COX-1, and human COX-2. In mouse neuronal HT22 cells, ML351 dose-dependently protected against oxidative glutamate toxicity and completely reversed the increase in 12-HETE following glutamate treatment [2][3].

In permanent focal ischemia mice model, IP administration of ML351 resulted in a ~30% reduction in infarct size [2][3].

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