Biochem/physiol Actions

Target IC₅₀: 180 nM against endothelial nitric oxide synthase (eNOS)

Reversible: no

Product does not compete with ATP.

Primary TargeteNOS

Cell permeable: yes

General description

A cell-permeable, irreversible endothelial nitric oxide synthase inhibitor. Inhibits iNOS in macrophages (IC₅₀ = 5 nM). Shown to inhibit acetylcholine-induced relaxation of preconstricted rat thoracic aortic rings (IC₅₀ = 180 nM). Blocks K⁺ and Ca²⁺ currents in arterial smooth muscle cells. Inhibitor of mitochondrial NADH-ubiquinone oxidoreductase. Inhibits other NADH utilizing flavoproteins, such as NADPH oxidase in human neutrophils and macrophages. Causes pressor and tachycardiac effects via indirect activation of the sympathetic nervous system.

A cell-permeable, irreversible inhibitor of endothelial nitric oxide synthase (eNOS). Shown to inhibit acetylcholine-induced relaxation of preconstricted rat thoracic aortic rings (IC₅₀ = 180 nM). Also inhibits iNOS in macrophages (IC₅₀ = 50 nM). Blocks K⁺ and Ca²⁺ currents in arterial smooth muscle cells. Inhibitor of mitochondrial NADPH-ubiquinone oxido-reductase.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Wang, Y.X., et al. 1995. Br. J. Pharmacol.114, 194.Majander, A., et al. 1994. J. Biol. Chem. 269, 21037.Weir, E.K., et al. 1994. J. Appl. Physiol. 76, 2611.Wang, Y.X., et al. 1993. Br. J. Pharmacol.110, 1232.Wang, Y.X., and Pang, C.C. 1993. Br. J. Pharmacol.109, 1186.Stuehr, D.J., et al. 1991. FASEB J.5, 98.Handcock, J.T., and Jones, O.T.G. 1987. Biochem. J.242, 103.

Packaging

10 mg in Plastic ampoule

Preparation Note

Slight warming is required for complete solubility.

Reconstitution

Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Warning

Toxicity: Carcinogenic / Teratogenic (D)