L-NAME HCl

Catalog No.S2877 Batch:S287707

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Technical Data

Formula

C7H15N5O4.HCl
Molecular Weight 269.69 CAS No. 51298-62-5
Solubility (25°C)* In vitro 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description 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.
Targets
nNOS [1]
(Cell-free assay)		 eNOS [1]
(Cell-free assay)
15 nM(Ki) 39 nM(Ki)
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. L-NAME 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 l-NAME in both cell types. [3]
In vivo L-NAME (0.03-300 mg kg-1, i.v.) induces a dose-dependent increase in mean systemic arterial blood pressure accompanied by bradycardia. L-NAME (100 mg kg-1, i.v.) inhibits significantly the hypotensive responses to ACh and bradykinin. The increase in blood pressure and bradycardia produced by L-NAME is reversed by L-arginine (30-100 mg kg-1, i.v.) in a dose-dependent manner. [2]

Protocol (from reference)

Kinase Assay:[1]
  • Enzyme Assay

    The oxidation of L-arginine 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.
Cell Assay:[3]
  • Cell lines

    rMC-1 cells

  • Concentrations

    1 mM

  • Incubation Time

    5 days

  • Method

    rMC-1 cells are incubated in 5 or 25 mM glucose, with or without l-NAME (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 inhibitor 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.

Animal Study:[2]
  • Animal Models

    Male Wistar rats

  • Dosages

    100 mg/kg

  • Administration

    i.v.

Customer Product Validation

, , 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.]

Selleck's L-NAME HCl has been cited by 42 publications

Piezo1 regulates meningeal lymphatic vessel drainage and alleviates excessive CSF accumulation [ Nat Neurosci, 2024, 10.1038/s41593-024-01604-8] PubMed: 38528202
Nitric oxide facilitates the S-nitrosylation and deubiquitination of Notch1 protein to maintain cancer stem cells in human NSCLC [ J Cell Mol Med, 2024, 28(21):e70203] PubMed: 39523215
Mitochondrial Hyperactivity and Reactive Oxygen Species Drive Innate Immunity to the Yellow Fever Virus-17D Live-Attenuated Vaccine [ bioRxiv, 2024, 2024.09.04.611167] PubMed: 39282299
Ginsenoside Rg1 attenuates diabetic vascular endothelial dysfunction by inhibiting the calpain-1/ROS/PKC-β axis [ Life Sci, 2023, 329:121972] PubMed: 37482213
NMDA receptor activation induces damage of alveolar type II cells and lung fibrogenesis through ferroptosis [ Biochim Biophys Acta Mol Cell Res, 2023, 1870(7):119535] PubMed: 37451346
Critical role of mitogen-inducible gene 6 in restraining endothelial cell permeability to maintain vascular homeostasis [ J Cell Commun Signal, 2023, 17(1):151-165] PubMed: 36284029
Critical role of mitogen-inducible gene 6 in restraining endothelial cell permeability to maintain vascular homeostasis [ J Cell Commun Signal, 2023, 17(1):151-165] PubMed: 36284029
Ginsenoside Rg1 ameliorates chronic intermittent hypoxia-induced vascular endothelial dysfunction by suppressing the formation of mitochondrial reactive oxygen species through the calpain-1 pathway [ J Ginseng Res, 2023, 47(1):144-154] PubMed: 36644390
Vitamin C deficiency induces hypoglycemia and cognitive disorder through S-nitrosylation-mediated activation of glycogen synthase kinase 3β [ Redox Biol, 2022, 56:102420] PubMed: 35969998
Suppression of VEGFD expression by S-nitrosylation promotes the development of lung adenocarcinoma [ J Exp Clin Cancer Res, 2022, 41(1):239] PubMed: 35941690

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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