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L-NAME hydrochloride (Synonyms: LNGNitroarginine methyl ester, N(G)-NitroL-arginine methyl ester)

カタログ番号GA11233

NG-ニトロ-L-アルギニンメチルエステル(L-NAME)は、異なる生物系において構成性一酸化窒素合成酵素(NOS)を抑制するために広く使用されています。

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L-NAME hydrochloride 化学構造

Cas No.: 51298-62-5

サイズ 価格 在庫数 個数
1g
$27.00
在庫あり
5g
$39.00
在庫あり
10g
$56.00
在庫あり
25g
$107.00
在庫あり
100g
$300.00
在庫あり

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Sample solution is provided at 25 µL, 10mM.

Product has been cited by 1 publications

Protocol

Cell experiment [1]:

Cell lines

Purified brain NOS

Preparation Method

L-NAME hydrochloride was added as 10 fold stock solutions of the respective hydrochlorides freshly prepared in water. For the bioactivation experiments aliquots of 10ul of the buffer,added to 90ul of the NOS reaction mixtures, yielding a theoretial final L-NAME concentration.

Reaction Conditions

0-1mM L-NAME hydrochloride for 24h

Applications

Freshly dissolved L-NAME was a inhibitor of purified brain NOS (mean IC50 = 70 μM), the apparent inhibitory potency of L-NAME approached that of L-NOARG upon prolonged incubation at neutral or alkaline pH.

Animal experiment [2]:

Animal models

Adult male Wistar rats (70–100 days of age) 

Preparation Method

Male Wistar rats were randomly assigned to control (C), L-NAME (L), chronic aerobic exercise (Ex), and chronic aerobic exercise associated to L-NAME (ExL). Aerobic training was performed with progressive intensity for 12 weeks; L-NAME was administered by orogastric gavage.

Dosage form

1.5 mg/kg/day L-NAME, oral gavage

Applications

Low-dose L-NAME alone did not change systolic blood pressure (SBP), but ExL significantly increased SBP at week 8 with normalization after 12 weeks. Furthermore, ExL promoted the elevation of left ventricle (LV) end-diastolic pressure without the presence of cardiac hypertrophy and fibrosis. Time to 50% shortening and relaxation were reduced in ExL, suggesting a cardiomyocyte contractile improvement. In conclusion, the association of chronic aerobic exercise and low-dose L-NAME prevented cardiac pathological remodeling and induced cardiomyocyte contractile function improvement

References:

[1]. Pfeiffer S, Leopold E, et al. Inhibition of nitric oxide synthesis by NG-nitro-L-arginine methyl ester (L-NAME): requirement for bioactivation to the free acid, NG-nitro-L-arginine. Br J Pharmacol. 1996 Jul;118(6):1433-40. 

[2]. Luchi TC, Coelho PM, et al. Lima-Leopoldo AP, Lunz W, Leopoldo AS. Chronic aerobic exercise associated to low-dose L-NAME improves contractility without changing calcium handling in rat cardiomyocytes. Braz J Med Biol Res. 2020 Mar 9;53(3):e8761.

Background

NG-ニトロ-L-アルギニンメチルエステル(L-NAME)は、異なる生物系において構成性NO合成酵素(NOS)を阻害するために広く使用されています。 L-NAMEは、一般的にNO欠乏性高血圧の誘導に使用されます[1]。

新鮮に溶解したL-NAMEは、精製された脳NOSの50倍低い抑制剤であった(平均IC50=70μM)。しかし、中性またはアルカリ性pHで長時間培養すると、L-NAMEの表面的な抑制効力はL-NOARGに近づいた。HPLC分析により、L-NAMEによるNOSの阻害作用が薬物をL-NOARGに加水分解することと密接に相関していることが明らかになった。[1]

IL-NAMEと関連化合物であるL-NA(100μM)は、自己収縮トーンを持つ加圧された血管(スプレーグ・ドーリーラット)を収縮させました。内皮の除去は収縮を引き起こすことはなく、自己収縮トーンも変化しませんでしたが、L-NAMEの収縮作用は持続しました。 L-arginine(1mM)によってL-NAMEの収縮作用が消失しました。[2]

References:
[1]: Pfeiffer S, Leopold E, et al. Inhibition of nitric oxide synthesis by NG-nitro-L-arginine methyl ester (L-NAME): requirement for bioactivation to the free acid, NG-nitro-L-arginine. Br J Pharmacol. 1996 Jul;118(6):1433-40.
[2].Murphy TV, Kotecha N, et al. Endothelium-independent constriction of isolated, pressurized arterioles by Nomega-nitro-L-arginine methyl ester (L-NAME). Br J Pharmacol. 2007 Jul;151(5):602-9. doi: 10.1038/sj.bjp.0707262. Epub 2007 Apr 30.

Chemical Properties

Cas No. 51298-62-5 SDF
同義語 LNGNitroarginine methyl ester, N(G)-NitroL-arginine methyl ester
Chemical Name methyl (2S)-2-amino-5-[[amino(nitramido)methylidene]amino]pentanoate;hydrochloride
Canonical SMILES COC(=O)C(CCCN=C(N)N[N+](=O)[O-])N.Cl
Formula C7H15N5O4.HCl M.Wt 269.7
溶解度 ≥ 27mg/mL in Water, ≥ 23 mg/mL in DMSO Storage Stored at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 3.7078 mL 18.5391 mL 37.0782 mL
5 mM 0.7416 mL 3.7078 mL 7.4156 mL
10 mM 0.3708 mL 1.8539 mL 3.7078 mL
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Related Video

    L-NAME hydrochloride-GlpBio

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