N-硝基-L-精氨酸甲酯作用机制 - Medchemexpress - MCE中国

1、Product Data SheetL-NAME hydrochlorideCat. No.: HY-18729ACAS No.: 51298-62-5分式: CHClNO分量: 269.69作靶点: NO Synthase作通路: Immunology/Inflammation储存式: Powder -20C 3 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 H2O : 125 mg/mL (463.50 mM; Need ultrasonic)DMSO : 100 mg/mL (370.80 mM; Need ultrasonic)H

2、2O : 32 mg/mL (118.65 mM)* means soluble, but saturation unknown.SolventMass1 mg 5 mg 10 mgConcentration制备储备液1 mM 3.7080 mL 18.5398 mL 37.0796 mL5 mM 0.7416 mL 3.7080 mL 7.4159 mL10 mM 0.3708 mL 1.8540 mL 3.7080 mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存式和期限：-80C, 6 months; -20C,

3、 1 month。-80C 储存时，请在 6 个内使，-20C 储存时，请在 1 个内使。BIOLOGICAL ACTIVITY物活性 L-NAME hydrochloride是NOS 的抑制剂，IC50 为70 M。IC & Target IC50: 70 M (NOS)1体外研究 L-arginine analogues are widely used inhibitors of nitric oxide synthase (NOS) activity, with Nw-nitro-L-argininemethyl ester (L-NAME) being at the head2. Fr

4、eshly dissolved L-NAME is a 50 fold less potent inhibitor of purifiedbrain NOS (mean IC50= 70 M) than L-NOARG (IC50= 1.4 M), but the apparent inhibitory potency of L-NAMEapproached that of L-NOARG upon prolonged incubation at neutral or alkaline pH. HPLC analyses reveal that NOSinhibition by L-NAME

5、closely correlated with hydrolysis of the drug to L-NOARG1.Page 1 of 2 www.MedChemE体内研究 L-NAME infusion significantly decreases NKT-leukocyte level, tumor-necrosis factor (TNF)-alpha production by T-splenocytes and macrophages, and interferon-gamma production by T-leukocytes, monocytes, and T-spleno

6、cytes, aswell as increased interleukin-6 production by T-leukocytes and monocytes and nitrate/nitrite production by T-leukocytes3. There is increasing evidence that nitric oxide may be involved in learning and memory. l-NAMEproduces a task-dependent impairment of fear extinction, and implies that ni

7、tric oxide signaling is involved inmemory process of certain fear extinction tasks4. Chronic L-NAME administration induces cardiac hypertrophy inrodent models. Six weeks L-NAME administration induces significant cardiac hypertrophy compared to control hearts5.PROTOCOLAnimal Rats: The purpose is to i

8、nvestigate dose effects of chronically infused NOS inhibitor, LNAME on the anabolism,Administration 35 inflammatory responses, and arginine metabolism in parenterally fed rats with cecal puncture-induced subacuteperitonitis. Male Wistar rats (8-9 weeks old), initially weighing 250 g, are used in the

9、 study. Rats are divided into 4groups and are administered total parenteral nutrition solutions with 0, 5 (low dose), 25 (medium dose), or 50 (highdose) mg/kg per day of L-NAME for 7 days3.Mice: 12-20 week old C57BL/6J mice (5 per group) are administered L-NAME (0.325mg/mL) in the drinking water.Hea

10、rts are excised at 1-day, 2-days, 5-days, 2-weeks or 6-weeks; or controls which received no L-NAME. Ventricularcross-sectional wall thickness and individual cardiac myocytes cross-sectional area and cardiomyocyte/nuclear ratioto determine cardiac hypertrophy. Immuno-histochemical staining for c-kit,

11、 sca-1 and BCRP undertaken5.MCE has not independently confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献 Arterioscler Thromb Vasc Biol. 2020 Apr 9:ATVBAHA120314172. Biomed Pharmacother. 2019 Jul;115:108934. Toxicol Appl Pharmacol. 2019 Mar 1;366:83-95. Mediat Inflamm. 2

12、019 Oct. Evid-Based Compl Alt. 2020 Mar.See more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Pfeiffer S, et al. Inhibition of nitric oxide synthesis by NG-nitro-L-arginine methyl ester (L-NAME): requirement forbioactivation to the free acid, NG-nitro-L-arginine. Br J Phar

13、macol. 1996 Jul;118(6):1433-40.2. Kopincov J, et al. L-NAME in the cardiovascular system - nitric oxide synthase activator? Pharmacol Rep. 2012;64(3):511-20.3. Lo HC, et al. The Nitric Oxide Synthase Inhibitor NG-Nitro-L-Arginine Methyl Ester Diminishes the Immunomodulatory Effects of Parental Argin

14、ine inRats with Subacute Peritonitis. PLoSOne. 2016 Mar 23;11(3):e0151973.4. Luo H, et al. Effect of nitric oxide synthase inhibitor L-NAME on fear extinction in rats: a task-dependent effect. Neurosci Lett. 2014 Jun 20;572:13-8.5. Ocsan RJ, et al. Chronic NG-nitro-l-arginine methyl ester (L-NAME) administration in C57BL/6J mice induces a sustained decrease in c-kit positive cellsduring development of cardiac hypertrophy. J Physiol Pharmacol. 2013 Dec;64(6):727-36.Page 2 of 3 www.MedChemEMc