Vanoxerine dihydrochloride (Synonyms: I 893) |
| Catalog No.GC17741 |
Le dichlorhydrate de vanoxérine (dichlorhydrate de GBR-12909) est un inhibiteur de la recapture de la dopamine compétitif, puissant et hautement sélectif (Ki = 1 nM).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 67469-78-7
Sample solution is provided at 25 µL, 10mM.
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Vanoxerine is an antagonist of dopamine transporter (DAT1) with Ki value of 16.9nM [1].
As an antagonist of DAT, vanoxerine is developed for treatment of Parkinson's disease and depression but has no effect on these diseases. Vanoxerine is also found to have desirable cardiac antiarrhythmic properties. It is a blocker of cardiac hERG (hKv11.1) with IC50 value of 0.84nM. It also blocks the ICa,L and hNav1.5 channel with IC50 values of 320nM and 830nM, respectively. Vanoxerine does not significantly prolong Purkinje fiber APD60 and APD90 and has no significant effect on QT or TDR. Further, the clinical trial demonstrates that the effective concentrations of vanoxerine are well tolerated and safe in man [2].
References:
[1] Giros B, el Mestikawy S, Godinot N, Zheng K, Han H, Yang-Feng T, Caron MG. Cloning, pharmacological characterization, and chromosome assignment of the human dopamine transporter. Mol Pharmacol. 1992 Sep;42(3):383-90.
[2] Lacerda AE, Kuryshev YA, Yan GX, Waldo AL, Brown AM. Vanoxerine: cellular mechanism of a new antiarrhythmic. J Cardiovasc Electrophysiol. 2010 Mar;21(3):301-10.
| Cas No. | 67469-78-7 | SDF | |
| Synonymes | I 893 | ||
| Chemical Name | 1-(2-(bis(4-fluorophenyl)methoxy)ethyl)-4-(3-phenylpropyl)piperazine dihydrochloride | ||
| Canonical SMILES | FC1=CC=C(C(OCCN2CCN(CC2)CCCC3=CC=CC=C3)C4=CC=C(F)C=C4)C=C1.Cl.Cl | ||
| Formula | C28H34Cl2F2N2O | M.Wt | 523.49 |
| Solubility | DMF: 2 mg/ml,DMSO: 2 mg/ml | 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 | 1.9103 mL | 9.5513 mL | 19.1026 mL |
| 5 mM | 0.3821 mL | 1.9103 mL | 3.8205 mL |
| 10 mM | 0.191 mL | 0.9551 mL | 1.9103 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 25 reference(s) in Google Scholar.)
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