L-NMMA acetate
(Synonyms: N-单甲基-L-精氨酸单乙酸酯,Tilarginine acetate; Methylarginine acetate) 目录号 : GC16926
L-NMMA acetate是一种强效一氧化氮合酶（NOS）抑制剂，IC50值为2μM。
Cas No.:53308-83-1
Sample solution is provided at 25 µL, 10mM.
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L-NMMA acetate is a potent inhibitor of Nitric-Oxide Synthase (NOS), with an IC50 of 2μM[1]. L-NMMA acetate has been widely used to regulate the vascular tension and blood pressure of arterial rings in animals[2].
In vitro, L-NMMA acetate treatment at 4000μM for 96 hours significantly reduced the proliferation and migration of the MDA-MB-231 and SUM159 cell lines[3]. L-NMMA acetate treatment (4000μM) for 72 hours inhibited the upregulation of inducible nitric oxide synthase (iNOS) induced by docetaxel in MDA-MB-468 cells and enhanced the Docetaxel-induced cell apoptosis[4]. L-NMMA acetate treatment (10000μM) for 42 hours significantly inhibited the expansion of porcine cumulus cells, without affecting nuclear or cytoplasmic maturation[5].
In vivo, L-NMMA acetate treatment via intravitreal injection (0.02μM/5μL; once every other day) for 4 weeks inhibited the NO signaling pathway and slowed down the progression of choroidal fibrosis in myopic guinea pigs[6]. In endotoxemic dogs, 22-hours intravenous infusion of L-NMMA acetate (10mg/kg/h) increased systemic and pulmonary vascular resistance, marginally increased mean arterial pressure, and decreased oxygen delivery[7].
References:
[1] Jung C S, Lange B, Zimmermann M, et al. Role of endogenous monomethylated L-arginine (L-NMMA) after subarachnoid hemorrhage[J]. Neurological Research, 2013, 35(7): 709-712.
[2] Rees D D, Palmer R M, Schulz R, et al. Characterization of three inhibitors of endothelial nitric oxide synthase in vitro and in vivo[J]. British journal of pharmacology, 1990, 101(3): 746.
[3] Granados-Principal S, Liu Y, Guevara M L, et al. Inhibition of iNOS as a novel effective targeted therapy against triple-negative breast cancer[J]. Breast Cancer Research, 2015, 17(1): 25.
[4] Dávila-González D, Choi D S, Rosato R R, et al. Pharmacological inhibition of NOS activates ASK1/JNK pathway augmenting docetaxel-mediated apoptosis in triple-negative breast cancer[J]. Clinical Cancer Research, 2018, 24(5): 1152-1162.
[5] Romero-Aguirregomezcorta J, Santa Á P, García-Vázquez F A, et al. Nitric oxide synthase (NOS) inhibition during porcine in vitro maturation modifies oocyte protein S-nitrosylation and in vitro fertilization[J]. PLoS One, 2014, 9(12): e115044.
[6] Li T, Bao B, Hao Y, et al. Suppressive effect of nitric oxide synthase (NOS) inhibitor L-NMMA acetate on choroidal fibrosis in experimental myopic guinea pigs through the nitric oxide signaling pathway[J]. European Journal of Pharmacology, 2023, 960: 176111.
[7] Cobb J P, Natanson C, Quezado Z M, et al. Differential hemodynamic effects of L-NMMA in endotoxemic and normal dogs[J]. American Journal of Physiology-Heart and Circulatory Physiology, 1995, 268(4): H1634-H1642.
L-NMMA acetate是一种强效一氧化氮合酶（NOS）抑制剂，IC50值为2μM[1]。L-NMMA acetate广泛应用于调节动物动脉环血管张力及血压[2]。
在体外，4000μM浓度的L-NMMA acetate处理96小时可显著抑制MDA-MB-231和SUM159细胞系的增殖与迁移[3]。4000μM浓度的L-NMMA acetate处理72小时能抑制多西他赛诱导的MDA-MB-468细胞中诱导型一氧化氮合酶（iNOS）上调，并增强多西他赛诱导的细胞凋亡[4]。10000μM浓度的L-NMMA acetate处理42小时可显著抑制猪卵丘细胞扩张，而不影响细胞核或细胞质成熟[5]。
在体内，玻璃体内注射0.02μM/5μL剂量的L-NMMA acetate（隔日一次，持续4周）可抑制NO信号通路，延缓近视豚鼠模型中的脉络膜纤维化进展[6]。在内毒素血症犬模型中，以10mg/kg/小时速率静脉输注L-NMMA acetate 22小时，可增加全身及肺血管阻力，轻微升高平均动脉压，并降低氧输送能力[7]。
| Cell experiment [1]: | |
Cell lines | MDA-MB-231 cells |
Preparation Method | MDA-MB-231 cells were maintained in Dulbecco's modified Eagle's medium (DMEM), supplemented with 10% fetal bovine serum and 1% antibiotic-antimycotic. Cells were treated daily with N-[[3-(aminomethyl)phenyl]methyl]-ethanimidamide (1000, 2000, 4000μM), L-NMMA acetate (1000, 2000, 4000μM) for 96 hours. The proliferation of MDA-MB-231 cell was determined by adding premixed WST-1 reagent. Confluent cells were treated in starvation conditions (1% serum) for 72 hours. The medium was then changed by regular growth medium in the presence of inhibitors for 24 hours. A 'wound' was made in the cell monolayer using a 100-μL pipette tip. Pictures were taken at 0 and 14 hours. Data were replicated in three independent experiments. |
Reaction Conditions | 1000, 2000, 4000μM; 96h |
Applications | L-NMMA acetate treatment significantly inhibited the proliferation and migration of the MDA-MB-231 cells. |
| Animal experiment [2]: | |
Animal models | Three-colored guinea pigs of British species |
Preparation Method | Clinical examinations before the experiment were performed to ensure that all guinea pigs did not have eye diseases, such as cataract, keratitis, and spontaneous myopia. The environment temperature of the laboratory was maintained at 25°C ± 2°C with a circadian rhythm of 12h/12h (day/night alteration). All the experimental guinea pigs were treated in accordance with the ethics for animal experiments and were guaranteed to have sufficient nutrient-rich feed every day. Fresh vegetables were supplemented to guinea pigs twice a day to provide vitamin C. The guinea pigs were divided into four groups (six animals in each group): a normal control (NC) group, a lens-induced myopia (LIM) group, a NOS inhibitor (L-NMMA acetate) injection group, and a NOS inhibitor solvent phosphate-buffered saline (PBS, pH7.2) group. The guinea pigs in the NC group were normally housed with no treatment, whereas the guinea pigs in the LIM group, L-NMMA group, and PBS group were fitted with −6.0D lenses on their right eyes to induce myopia. The pigs in the L-NMMA acetate group received 5μL (0.02μM) of L-NMMA acetate once every other day (3 times a week) through an intravitreal injection, and the pigs in the PBS group received only 5μL of sterilized 1 × PBS. To ensure the success of the experiment, all the lenses were cleaned every morning and evening, and replaced immediately if scratches appeared. After 4 weeks of myopia induction, 3 guinea pigs in each group were randomly selected and anesthetized with 10g/L of pentobarbital sodium by intraperitoneal injection. The blood and hair of guinea pig were rinsed with sterile 0.9% NaCl solution. Subsequently, the fascial tissues around the eye were carefully peeled off by sterile ophthalmic scissors and the eyeball was taken out immediately and put into the sampling tube containing fixative solution for 24h of routine dehydration. Next, paraffin embedding was processed and sectioned into 3-μm sections for histopathological assessment and Masson Staining. |
Dosage form | 0.02μM/5μL, once every other day for 4 weeks; intravitreal injection |
Applications | L-NMMA acetate treatment significantly alleviated choroidal fibrosis in myopic guinea pigs. |
References: | |
| Cas No. | 53308-83-1 | SDF | |
| 别名 | N-单甲基-L-精氨酸单乙酸酯,Tilarginine acetate; Methylarginine acetate | ||
| 化学名 | (S,E)-2-amino-5-(2-methylguanidino)pentanoic acid compound with acetic acid (1:1) | ||
| Canonical SMILES | OC([C@H](CCCN/C(N)=N/C)N)=O.OC(C)=O | ||
| 分子式 | C7H16N4O2.CH3CO2H | 分子量 | 248.28 |
| 溶解度 | DMSO: .25 mg/ml,Ethanol: 1 mg/ml,PBS (pH 7.2): 10 mg/ml | 储存条件 | Store 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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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.0277 mL | 20.1386 mL | 40.2771 mL |
| 5 mM | 0.8055 mL | 4.0277 mL | 8.0554 mL |
| 10 mM | 0.4028 mL | 2.0139 mL | 4.0277 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.
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- Purity: >98.00%
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