HET0016 (339068-25-6) inhibits 20-hydroxyeicosatetraenoic acid (20-HETE) biosynthesis via omega oxidation of arachidonic acid mediated by CYP4A and 4F (IC50=8.9 nM in human renal microsomes).1 It displays neuroprotective effects in a rat model of traumatic brain injury via inhibition of neuronal pyroptosis.2 HET0016 attenuates cerebral ischemia-reperfusion injury3 as well as oxidative injury and peripheral nerve damage in type-2 diabetic mice4. It alleviates myocardial oxidative stress5 and restores endothelial function suggesting therapeutic potential in obesity-associated vascular disease6.
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