Product Information
- HET-0016
- methanimidamide, N'-(4-butyl-2-methylphenyl)-N-hydroxy-
- N-(4-butyl-2-methylphenyl)-N'-hydroxyiminoformamide
Applications 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).
References Miyata, N., et al.: Br. J. Pharmacol., 133, 325 (2001), Amaral, S.L., et al.: Am. J. Physiol. Heart Circ. Physiol., 284, H1528 (2003), Mulligan, S.J. and MacVicar, B.A.: Nature, 431, 195 (2004), Poloyac, S.M., et al.: J. Ceteb. Blood Flow Metab., March 29, (2006) in Press