Vinyl-L-NIO (hydrochloride) |
| Catalog No.GC12928 |
potent, selective inhibitor of nNOS
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 728944-69-2
Sample solution is provided at 25 µL, 10mM.
;)
_1-7.$$$37316672@70.jpg');)
;)
;)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
;)
;)
;)
_1124-1138.$$$35908550@30.jpg');)
_766-780.$$$37100057@30.jpg');)
_418-432.$$$36893736@30.jpg');)
_240-255.$$$35108512@29.jpg');)
_533-545.$$$36543525@28.jpg');)
_264-276.$$$36600053@22.jpg');)
_2214998.$$$@0.jpg');)
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 | |
| Chemical Name | N5-(1-imino-3-butenyl)-L-ornithine, monohydrochloride | ||
| Canonical SMILES | C=CCC(NCCC[C@H](N)C(O)=O)=N.Cl | ||
| Formula | C9H17N3O2 • HCl | M.Wt | 235.7 |
| Solubility | ≤30mg/ml in ethanol;50mg/ml in DMSO;50mg/ml in dimethyl formamide | 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. |
||
| 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 | 4.2427 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 |
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 22 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *