Tetrabenazine Racemate
Based on 1 Customer Validation
Tetrabenazine (Ro 1-9569) Racemate is a brain-penetrant and orally active VMAT2-selective ligand with human VMAT2 Ki 100 nM. Tetrabenazine Racemate binds VMAT2 to block monoamine uptake into synaptic vesicles, potentiates cytoplasmic monoamine degradation. Tetrabenazine Racemate weakly blocks dopamine D2 receptors, and increases dopamine turnover via elevated cerebrospinal fluid homovanillic acid. Tetrabenazine Racemate can be used for the research of Huntington’s disease, tardive dyskinesia, and Tourette’s syndrome.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.89%
- CAS. Nr.: 718635-93-9
- Formel: C19H27NO3
- Molecular Weight:317.42
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Chemical Information
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Lösungsmittel & Löslichkeit
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Biologische Aktivität
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D2 Receptor ~2.1 μM (Ki) |
Tetrabenazine Racemate reversibly inhibits human VMAT2 with a Ki of ~100 nM, reducing monoamine uptake into synaptic vesicles and depleting presynaptic monoamine stores[1].
Tetrabenazine Racemate inhibits dopamine D2 receptors in striatal membranes with a Ki of ~2.1 μM[1].
Tetrabenazine Racemate (0.3-10.0 μg/mL; 4 h) releases serotonin from rabbit blood platelets in vitro in a concentration-dependent manner[3].
Tetrabenazine Racemate (5-20 mg/L) is 60% bound to nondiffusible components of rabbit plasma[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Tetrabenazine Racemate (7 days) causes irreversible locomotor changes and substantia nigra pars compacta neuronal damage in healthy rats[1].
Tetrabenazine Racemate (50-150 mg/kg; i.v.; daily for 3-9 days) exhibits short-lived, central nervous system-selective Reserpine (HY-N0480)-like effects in rabbits[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:New Zealand White male (~2 kg)[3]
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Dosage:50 mg/kg; 150 mg/kg
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Administration:i.v.; daily for 3, 7, 9 days
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Result:Decreased brain serotonin to ~50% of normal within 1 hour, remained at this level for several hours, and returned to near normal by 18-24 hours.
Declined brain norepinephrine to ~15% of normal over 4 hours, and returned to ~70% of normal by 24 hours.
Did not measurably affect peripheral serotonin in blood platelets and small intestine, and norepinephrine in heart.
Caused <10% depletion of adrenal catecholamines at 4 hours and ~40% depletion at 24 hours.
Reduced plasma drug levels to <3 μg/mL by 6 hours, and made them undetectable by 24 hours.
Reached brain drug levels of ~45 μg/g within 10 minutes, declined to ~1.3 μg/g by 6 hours, and made them undetectable by 24 hours.
Failed to affect intestinal/platelet serotonin or heart norepinephrine, but caused 50% depletion of adrenal catecholamines by the end of infusion with single 150 mg/kg i.v. dose.
Showed no drug accumulation in plasma or tissues 24 hours after the last dose with repeated 50 mg/kg daily i.v. doses.
Chemical Information
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CAS. Nr. 718635-93-9
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Appearance Solid
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Molecular Weight 317.42
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Formel C19H27NO3
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Color White to light yellow
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SMILES
O=C1C(CC(C)C)CN2CCC3=CC(OC)=C(OC)C=C3C2C1
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Synonyms
Ro 1-9569 Racemate
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Lösungsmittel & Löslichkeit
DMSO : 50 mg/mL (157.52 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.88 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (7.88 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Reinheit & Dokumentation
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Data Sheet (288 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Fasano A, et al. Tetrabenazine. Expert Opin Pharmacother. 2009 Dec;10(17):2883-96. [Content Brief]
[2]. Jankovic J. Tetrabenazine in the treatment of hyperkinetic movement disorders. Adv Neurol. 1983;37:277-89. [Content Brief]
[3]. QUINN GP, et al. Biochemical and pharmacological studies of RO 1-9569 (tetrabenazine), a nonindole tranquilizing agent with reserpine-like effects. J Pharmacol Exp Ther. 1959 Oct;127:103-9. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.1504 mL | 15.7520 mL | 31.5040 mL | 78.7600 mL |
| 5 mM | 0.6301 mL | 3.1504 mL | 6.3008 mL | 15.7520 mL | |
| 10 mM | 0.3150 mL | 1.5752 mL | 3.1504 mL | 7.8760 mL | |
| 15 mM | 0.2100 mL | 1.0501 mL | 2.1003 mL | 5.2507 mL | |
| 20 mM | 0.1575 mL | 0.7876 mL | 1.5752 mL | 3.9380 mL | |
| 25 mM | 0.1260 mL | 0.6301 mL | 1.2602 mL | 3.1504 mL | |
| 30 mM | 0.1050 mL | 0.5251 mL | 1.0501 mL | 2.6253 mL | |
| 40 mM | 0.0788 mL | 0.3938 mL | 0.7876 mL | 1.9690 mL | |
| 50 mM | 0.0630 mL | 0.3150 mL | 0.6301 mL | 1.5752 mL | |
| 60 mM | 0.0525 mL | 0.2625 mL | 0.5251 mL | 1.3127 mL | |
| 80 mM | 0.0394 mL | 0.1969 mL | 0.3938 mL | 0.9845 mL | |
| 100 mM | 0.0315 mL | 0.1575 mL | 0.3150 mL | 0.7876 mL |
Tetrabenazine Racemate Related Classifications
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