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.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
eNOS
Product does not compete with ATP.
Reversible: no
Target IC50: 180 nM against endothelial nitric oxide synthase (eNOS)
Warning
Toxicity: Carcinogenic / Teratogenic (D)
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.
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.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
- UPC:
- 51282533
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 300260-10MG