L-NAME hydrochloride
(Synonyms: N'-硝基-L-精氨酸甲酯盐酸盐,L-NAME, L-NAME HCL) 目录号 : GA11233
NG-硝基-L-精氨酸甲酯 (L-NAME) 已广泛用于抑制不同生物系统中的组成型一氧化氮合酶 (NOS)。
Cas No.:51298-62-5
Sample solution is provided at 25 µL, 10mM.
NG-nitro-L-arginine methyl ester (L-NAME) have been widely used to inhibit constitutive NO synthase (NOS) in different biological systems. L-NAME commonly used for the induction of NO-deficient hypertension[1].
Freshly dissolved L-NAME was a 50 fold less potent inhibitor of purified brain NOS (mean IC50 = 70 μM) than L-NOARG (IC50 = 1.4 μM), but the apparent inhibitory potency of L-NAME approached that of L-NOARG upon prolonged incubation at neutral or alkaline pH. HPLC analyses revealed that NOS inhibition by L-NAME closely correlated with hydrolysis of the drug to L-NOARG[1].
IL-NAME and the related compound L-NA (100 μM) constricted pressurized vessels (Sprague–Dawley rats) with myogenic tone. Removal of the endothelium did not cause constriction or alter myogenic tone, however the constrictor effect of L-NAME persisted. The constrictor effect of L-NAME was abolished by L-arginine (1 mM)[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.
NG-硝基-L-精氨酸甲酯 (L-NAME) 已广泛用于抑制不同生物系统中的组成型一氧化氮合酶 (NOS)。 L-NAME 通常用于诱导 NO 缺乏型高血压[1]。
与 L-NOARG（IC50 = 1.4）相比，新鲜溶解的 L-NAME 对纯化脑 NOS 的抑制作用（平均 IC50 = 70 μM）低 50 倍μM)，但在中性或碱性 pH 条件下长时间孵育后，L-NAME 的表观抑制效力接近 L-NOARG。 HPLC 分析表明，L-NAME 对 NOS 的抑制作用与药物水解为 L-NOARG 密切相关[1]。
IL-NAME 和相关化合物 L-NA (100 μM) 收缩具有生肌张力的加压血管（Sprague-Dawley 大鼠）。去除内皮不会引起收缩或改变肌原性张力，但 L-NAME 的收缩效应仍然存在。 L-NAME 的收缩作用被 L-精氨酸 (1 mM)[2] 消除。
| Cell experiment [1]: | |
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Cell lines |
Purified brain NOS |
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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. |
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Reaction Conditions |
0-1mM L-NAME hydrochloride for 24h |
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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]: | |
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Animal models |
Adult male Wistar rats (70–100 days of age) |
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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. |
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Dosage form |
1.5 mg/kg/day L-NAME, oral gavage |
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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 |
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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. |
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| Cas No. | 51298-62-5 | SDF | |
| 别名 | N'-硝基-L-精氨酸甲酯盐酸盐,L-NAME, L-NAME HCL | ||
| 化学名 | 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 | ||
| 分子式 | C7H15N5O4.HCl | 分子量 | 269.7 |
| 溶解度 | ≥ 27mg/mL in Water, ≥ 23 mg/mL in DMSO | 储存条件 | Stored at -20°C |
| General tips | 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；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
