Nω-ニトロ-L-アルギニンメチル塩酸塩

用途NO合成酵素(NOS)阻害剤、NOの生体内での生理活性発現機構の解析。

説明L-NAME requires hydrolysis of the methyl ester by cellular esterases to become a fully functional inhibitor (L-NNA). L-NNA exhibits some selectivity for inhibition of neuronal and endothelial isoforms. It exhibits Ki values of 15 nM, 39 nM, and 4.4 μM for nNOS (bovine), eNOS (human), and iNOS (mouse), respectively. The reported Ki value for the inhibition of iNOS ranges from 4-65 μM. L-NAME inhibits cGMP formation in endothelial cells with an IC50 of 3.1 μM (in the presence of 30 μM arginine) and reverses the vasodilation effects of acetylcholine in rat aorta rings with an EC50 of 0.54 μM.

使用Nitroarginine Methyl Ester Hydrochloride is used in the synthesis of N/CD13 inhibitors playing an important role in tumor invasion, metastatsis and angiogenesis. Also used in the preparation of spirocyclic lactam as a type II’ β-turn inducer.

一般的な説明More soluble analog of arginine and a competitive, slowly reversible inhibitor of endothelial nitric oxide synthase (IC50 = 500 nM). Causes a prolonged inhibition of acetylcholine-induced relaxation of rat aortic rings (IC50 = 400 nM).