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L-NAME HCl

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Chemical Structure| 51298-62-5 同义名 : NG-Nitroarginine methyl ester hydrochloride;L-NAME (hydrochloride);H-Arg(NO2)-OMe.HCl;51298-62-5;N(G)-Nitro-L-arginine methyl ester;L-NG-Nitroarginine methyl ester;N-Nitro-L-arginine methylester;NG-Nitroarginine methyl ester;L-NAME HCl
CAS号 : 51298-62-5
货号 : A135741
分子式 : C7H16ClN5O4
纯度 : 98%
分子量 : 269.686
MDL号 : MFCD00039052
存储条件：

粉末 Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(389.34 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 100 mg/mL(370.8 mM)，配合低频超声助溶
动物实验配方：
生物活性
靶点

  • eNOS

    eNOS, Ki:39 nM

  • iNOS

    iNOS, Ki:4.4 μM

  • nNOS

    nNOS, Ki:15 nM
描述 Nitric oxide synthase (NOS) is an enzyme responsible for the production of nitric oxide (NO) from L-arginine. L-NAME HCl is an inhibitor for bovine brain NOS and mouse macrophage NOS with Ki values of 15 nM and 4.4 μM, respectively[1]. In rMC-1 cells, the accumulation of NO induced by glucose (25 mM) was inhibited by 1 mM L-NAME HCl. The treatment of L-NAME HCl at 1 mM also led to significantly decreased cell death in glucose-stimulated rMC-1 cells. Elevated production of PGE2 in BREC cells was significantly suppressed by 1 mM L-NAME HCl[2]. With the presence of 30 μM L-arginine and 100 μM NADPH, L-NAME HCl at 0.1 – 100 μM dose-dependently inhibited the formation of cyclic GMP in endothelial cytosol with an IC50 value of 3.1 μM. It also inhibited [3H]-citrulline formation with an IC50 value of 0.09 μM. L-NAME HCl at 0.1 – 300 μM induced endothelium-dependent contraction of rings of rat aorta with an EC50 value of 26 μM in the presence of 10 nM phenylephrine. The relaxation of rings of rat aorta was inhibited by 0.1 – 10 μM L-NAME HCl at a dose-dependent manner with an IC50 value of 0.54 μM. In Wistar rats, i.v. administration of L-NAME HCl (0.03 – 300 mg/kg) dose-dependently increased the mean arterial blood pressure with an EC50 value of 2.4 mg/kg, and the highest blood pressure induced by L-NAME HCl was 44.1 mmHg. The same treatment of L-NAME HCl also resulted in bradycardia at a concentration-dependent manner[3].
作用机制 L-NAME HCl is a soluble methyl ester that inhibits NOS. Intracellular esterases convert a variable and unknown fraction of L-NAME to L-NNA, which tightly but reversibly binds to NOS, competing with L-arginine[4].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
mouse BV2 cells Function assay 24 h Inhibition of Nitric oxide synthase activity in mouse BV2 cells assessed as LPS-induced NO production after 24 hrs by Griess reaction, IC50=18.9 μM 21377368
mouse RAW264.7 cells Function assay 17-20 h Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of IFN-gamma/LPS-stimulated nitric oxide production after 17 to 20 hrs by Griess assay, IC50=27.13 μM 19359068
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.71mL

0.74mL

0.37mL

18.54mL

3.71mL

1.85mL

37.08mL

7.42mL

3.71mL
参考文献

[1]Furfine ES, Harmon MF, et al. Selective inhibition of constitutive nitric oxide synthase by L-NG-nitroarginine. Biochemistry. 1993;32(33):8512-7.

[2]Du Y, Sarthy VP, Kern TS. Interaction between NO and COX pathways in retinal cells exposed to elevated glucose and retina of diabetic rats. Am J Physiol Regul Integr Comp Physiol. 2004;287(4):R735-41.

[3]Rees DD, Palmer RM, et al. Characterization of three inhibitors of endothelial nitric oxide synthase in vitro and in vivo. Br J Pharmacol. 1990;101(3):746-52.

[4]Griffith OW, Kilbourn RG. Nitric oxide synthase inhibitors: amino acids. Methods Enzymol. 1996.