HET-0016 is a potent and selective inhibitor of the biosynthesis of 20-HETE acting via inhibition of CYP4A (IC50=8.9nM (human), 35nM (rat renal microsome). IC50 cyclooxygenase=2.3uM. IC50 for other CYP’s: CYP2C9-3.3uM, CYP2D6=83.9 uM, CYP3A4=71uM. It inhibits cerebrovascular constriction induced by Ca2+ or archidonate and inhibits angiogenesis and endothelial cell sprouting in various models. Displays protective effect on brain damage after temporary focal ischemia (at 10mg/Kg).
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