L-NAME HCl

製品コードS2877 バッチS287707

印刷

化学情報

Chemical Structure Synonyms NG-Nitroarginine methyl ester, N-Nitro-L-arginine methylester Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C7H15N5O4.HCl
分子量 269.69 CAS No. 51298-62-5
Solubility (25°C)* 体外 Water 54 mg/mL (200.22 mM)
DMSO Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 L-NAME HCl (NG-Nitroarginine methyl ester, N-Nitro-L-arginine methylester) is a nonselective inhibitor of nitric oxide synthetases (NOS) for nNOS (bovine), eNOS (human), and iNOS (murine), with Ki of 15 nM, 39 nM and 4.4 μM, respectively. L-NAME HCl can be used to induce animal models of Hypertension.
in vitro NG-nitro-L-arginine methyl ester (L-NAME; at 0.1-100 mM) causes concentration-dependent inhibition of the Ca2(+)-dependent endothelial NO synthase from porcine aortae. This compound causes an endothelium-dependent contraction and an inhibition of the endothelium-dependent relaxation induced by acetylcholine (ACh) in aortic rings. [2] In another research, Viability of rMC-1 cells or BREC in 25 mM glucose is significantly less than at 5 mM glucose, and this cell death is inhibited by this chemical in both cell types. [3]
in vivo L-NAME HCl (0.03-300 mg kg-1, i.v.) induces a dose-dependent increase in mean systemic arterial blood pressure accompanied by bradycardia. This compound (100 mg kg-1, i.v.) inhibits significantly the hypotensive responses to ACh and bradykinin. The increase in blood pressure and bradycardia produced by this chemical is reversed by L-arginine (30-100 mg kg-1, i.v.) in a dose-dependent manner. [2]

プロトコル(参考用のみ)

キナーゼアッセイ Enzyme Assay
The oxidation of L-NAME HCl (Nω-nitro-L-arginine methyl ester hydrochloride) is monitored by the conversion of [3H]- or [14C]-arginine to L-citrulline which separates L-citrulline from L-arginine by Dowex 50x8-200 (Na) chromatography. Typical reaction mixtures (100 pL) contains 50 mM HEPES, pH 7.0, 8 pM tetrahydrobiopterin, 1 mM CaC12, 0.01 mg/mL calmodulin, 0.5 mM EDTA, 0.450 pM [14C]-arginine (30000 cpm), and 100-200 pM NADPH. The cNOS-catalyzed oxidation of NADPH to NADP+ is monitored by the reduction of absorbance at 340 nm with a Kontron 860 spectrophotometer in a volume of 300 pL. All reactions are at 30 ℃ unless otherwise indicated.
細胞アッセイ 細胞株 rMC-1 cells
濃度 1 mM
反応時間 5 days
実験の流れ rMC-1 cells are incubated in 5 or 25 mM glucose, with or without L-NAME HCl (1 mM). Media is changed every other day for up to 5 days. BREC cells are incubated in 5 or 25 mM glucose as well as this compound as described above for 5 days. Cell death is determined by light microscopy using a hemocytometer and a 0.4% trypan blue dye exclusion method. The number of cells that do not exclude the dye is expressed per 1,000 total cells. A minimum of 800 cells is counted per assay (8 dishes, >100 cells counted per dish), and the assay is replicated three times on different days.
動物実験 動物モデル Male Wistar rats
投薬量 100 mg/kg
投与方法 i.v.

参考

  • https://pubmed.ncbi.nlm.nih.gov/7689333/
  • https://pubmed.ncbi.nlm.nih.gov/1706208/
  • https://pubmed.ncbi.nlm.nih.gov/15371279/
  • https://pubmed.ncbi.nlm.nih.gov/9395704/

カスタマーフィードバック

, , Cancer Biol Ther, 2014, 15(6):758-67.

, , Biochem Biophys Res Commun, 2015, 465(4):803-9.

Data from [Data independently produced by , , Front Plant Sci, 2016, 7:1652.]

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人間や獣医の診断であるか治療的な使用のためにでない。

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