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L-NIO dihydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
L-NIO dihydrochloride图片
CAS NO:159190-44-0
包装与价格:
包装价格(元)
10mg电议
50mg电议

产品介绍
L-NIO dihydrochloride 是一种有效、非选择性和 NADPH 依赖性一氧化氮合酶 (NOS) 抑制剂,对神经元 (nNOS)、内皮细胞 (eNOS) 和诱导型 (iNOS) 的 Kis 分别为 1.7、3.9、3.9 μM 。
Cas No.159190-44-0
化学名(S,E)-2-amino-5-((1-aminoethylidene)amino)pentanoic acid dihydrochloride
Canonical SMILESOC([C@H](CCC/N=C(C)/N)N)=O.Cl.Cl
分子式C7H15N3O2.2HCl
分子量246.13
溶解度<24.61mg/ml in Water
储存条件Desiccate at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

IC50: 65 M

L-NIO dihydrochloride is an inhibitor of nitric oxide (NO) synthase (iNOS, eNOS and nNOS). An NO synthase is inducible by immunological stimuli such as endotoxin (LPS) and various cytokines, generating nitric oxide (NO) in phagocytic cells including neutrophils and macrophages. Generation of NO by macrophages has been revealed to kill tumour cells due to the inactivation of ironsulphur centres of mitochondrial enzymes.

In vitro: To protect against inflammatory injury stimulated by activated neutrophils, the ability of L-arginine (N-iminoethyl-L-ornithine (L-NIO) was studied in rats, following intradermal or intrapulmonary deposition of immune complexes [1]. The protective effect of L-NIO in the skin was reversed in a dose-dependent manner by the presence of L-arginine, rather than by D-arginine. The protective effects of L-NIO L-Arginine were reversed also in immune complex-induced lung injury, and not associated with reductions in neutrophil accumulation as measured by extraction from tissues of myeloperoxidase. The results demonstrate immune complex induced vascular injury induced by activated macrophage was inhibited effectively by L-NIO as a potent inhibitor [1].

In vivo: A dose-dependent increase in mean systemic arterial blood pressure accompanied by bradycardia was induced at the administration of L-NIO (0.03-300 mgkg-1, i.v.). L-NIO (100 mgkg-, i.v.) has an effect inhibitor of the hypotensive responses to ACh and bradykinin. L-arginine (30-100 mg kg- 1, i.v.) in a dose-dependent manner reversed the increase in blood pressure and bradycardia produced by these compounds. It was enantiomer specific for all of these effects. These facts indicate that L-NIO can inhibit NO synthase as inhibitors in the vascular endothelium and verify that L-NIO plays an important role for NO synthesis in the maintenance of vascular tone and blood pressure [2].

Clinical trial: So far, no clinical study has been conducted.

References:
[1].  Mulligan MS, Moncada S, Ward PA. Protective effects of inhibitors of nitric oxide synthase in immune complex-induced vasculitis. Br J Pharmacol. 1992 Dec;107(4):1159-62.
[2].  Rees DD, Palmer RM, Schulz R, Hodson HF, Moncada S.Br J Pharmacol. Characterization of three inhibitors of endothelial nitric oxide synthase in vitro and in vivo.1990 Nov;101 (3):746-52.