Biochem/physiol Actions

Reversible: no

Product does not compete with ATP.

Target IC₅₀: 500 nM against endothelial nitric oxide synthase (eNOS); 2 µM against acetylcholine-induced relaxation of rat aorta rings; EC50 = 19.5 mg/kg for a dose-dependent increase in mean arterial blood pressure in the rat

Primary TargeteNOS

Cell permeable: yes

General description

A cell-permeable, more potent inhibitor of endothelial nitric oxide synthase (eNOS; IC₅₀ = 500 nM) compared to other arginine analogs such as L-NAME (Cat. No. 483125) and L-NMMA (Cat. No. 475886). Inhibits acetylcholine-induced relaxation of rat aorta rings (IC₅₀ = 2 µM) and causes a dose-dependent increase in mean arterial blood pressure in the rat (EC₅₀ = 19.5 mg/kg).

Cell permeable. Approximately five times more potent as an inhibitor of endothelial nitric oxide synthase (IC₅₀ = 500 nM) than other arginine analogs, such as L-NAME (Cat. No. 483125) and L-NMMA (Cat. No. 475886). Inhibits acetylcholine induced relaxation of rat aorta rings (IC₅₀ = 2 µM) and causes a dose-dependent increase in mean arterial blood pressure in the rat (EC₅₀ = 19.5 mg/kg).

Legal Information

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

Other Notes

Moore, W.M., et al. 1994. J. Med. Chem. 37, 3886.Rees, D.D., et al. 1990. Br. J. Pharmacol.101, 746.

Packaging

20 mg in Plastic ampoule

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 2 months at -20°C.

Warning

Toxicity: Irritant (B)