Vinyl-L-NIO (hydrochloride)
目录号 : GC12928
A potent, selective nNOS inhibitor
Cas No.:728944-69-2
Sample solution is provided at 25 µL, 10mM.
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IC50: 100 nM, 12 and 60 μM for nNOS, eNOS, and iNOS, respectively
Vinyl-L-NIO is a potent and selective inhibitor of nNOS.
Nitric oxide synthase (NOS) catalyzes the NADPH- and O2-dependent conversion of L-arginine to nitric oxide (NO) and citrulline. Three isoforms including the neuronal (nNOS), endothelial, and inducible have currently been identified. Since NO overproduction is able to contribute to various pathophysiological conditions, NOS inhibitors are considered as potential therapeutic agents.
In vitro: Vinyl-L-NIO was identified as a potent and selective inhibitor of nNOS. The Ki values for inhibition of nNOS, eNOS, and iNOS are 100 nM, 12 and 60 μM, respectively, as determined using initial rate measurements. Moreove, vinyl-L-NIO could irreversibly inactivate nNOS with a kinact of 0.078 min-1 and a Ki value of 90 nM in the presence of NADPH and O2. In additioin, it was found that vinyl-L-NIO was not able to inactivate iNOS and eNOS needed 20-fold higher concentrations of vinyl-L-NIO to achive 75% the rate of inactivation seen with nNOS [1].
In vivo: Vinyl-L-NIO was intracerebroventricularly injected at a dose of 10 microg/rat just before intraperitoneal injection of LPS. Vinyl-L-NIO injected at a selected doses had no effect on normal day-time body temperature and normal night-time. Vinyl-L-NIO at a dose of 10 microg/animal could suppress the LPS-induced fever in rats. The fever index calculated for rats pretreated with vinyl-L-NIO was reduced by 43%, compared to that calculated for water-pretreated and LPS-injected rats [2].
Clinical trial: So far, no clinical study has been conducted.
References:
[1] Babu, B. R., and Griffith, O.W. N5-(1-Imino-3-butenyl)-L-ornithine. A neuronal isoform selective mechanism-based inactivator of nitric oxide synthase. The Journal of Biological Chemisty 273, 8882-8889 (1998).
[2] Soszynski D, Chelminiak M. Intracerebroventricular injection of neuronal and inducible nitric oxide synthase inhibitors attenuates fever due to LPS in rats. J Physiol Pharmacol. 2007 Sep;58(3):551-61.
| Cas No. | 728944-69-2 | SDF | |
| 化学名 | N5-(1-imino-3-butenyl)-L-ornithine, monohydrochloride | ||
| Canonical SMILES | C=CCC(NCCC[C@H](N)C(O)=O)=N.Cl | ||
| 分子式 | C9H17N3O2 • HCl | 分子量 | 235.7 |
| 溶解度 | ≤30mg/ml in ethanol;50mg/ml in DMSO;50mg/ml in dimethyl formamide | 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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| 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 | 4.2427 mL | 21.2134 mL | 42.4268 mL |
| 5 mM | 0.8485 mL | 4.2427 mL | 8.4854 mL |
| 10 mM | 0.4243 mL | 2.1213 mL | 4.2427 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