Methyl-L-NIO (hydrochloride) |
| Catalog No.GC15360 |
competitive nitric oxide synthase (NOS) inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 150403-96-6
Sample solution is provided at 25 µL, 10mM.
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Ki: 3.0 μM for nNOS; 10.0 μM for eNOS; 9.5 μM for iNOS
Methyl-L-NIO is a competitive nitric oxide synthase (NOS) inhibitor.
Nitric oxide synthase (NOS) catalyzes the NADPH- and O2-dependent conversion of L-arginine to nitric oxide (NO). Three isoforms, the neuronal (nNOS), endothelial, and inducible, have been identified. Since NO overproduction contributes to various pathophysiological conditions, NOS inhibitors are considered as potential therapeutic agents.
In vitro: Previous study found that both methyl-L-NIO and its close analog ethyl-L-NIO were more potent inhibitors of nNOS than of eNOS or iNOS. However, expressed on a Ki/Km basis, neither of these two inhibitors showed biologically significant selectivity for nNOS over eNOS. In fact, both compounds showed a very modest selectivity for iNOS over the constitutive isoforms. In addition, methyl-L-NIO required a 10-fold higher concentration to duplicate the inactivation seen with L-NIO. Further extension to form the saturated analog of L-VNIO such as ethyl-L-NIO led to an inactivation of nNOS under the conditions examined [1].
In vivo: Up to now, there is no animal in vivo data reported.
Clinical trial: So far, no clinical study has been conducted.
Reference:
[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).
| Cas No. | 150403-96-6 | SDF | |
| Chemical Name | N5-(1-iminopropyl)-L-ornithine, monohydrochloride | ||
| Canonical SMILES | CCC(NCCC[C@H](N)C(O)=O)=N.Cl | ||
| Formula | C8H17N3O2 • HCl | M.Wt | 223.7 |
| Solubility | ≤10mg/ml in PBS | Storage | Store 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. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 4.4703 mL | 22.3514 mL | 44.7027 mL |
| 5 mM | 0.8941 mL | 4.4703 mL | 8.9405 mL |
| 10 mM | 0.447 mL | 2.2351 mL | 4.4703 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 31 reference(s) in Google Scholar.)
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