1. Membrane Transporter/Ion Channel
  2. Monoamine Transporter
  3. Tetrabenazine

Tetrabenazine  (Synonyms: Ro 1-9569)

Cat. No.: HY-B0590 Purity: 98.23%
COA Handling Instructions

Tetrabenazine (Ro 1-9569) is a reversible inhibitor of the vesicular monoamine transporter VMAT2 with the Kd value of 1.34 nM. Tetrabenazine can be used for research on diseases related to hyperactive movement disorders such as Huntington's disease.

For research use only. We do not sell to patients.

Tetrabenazine Chemical Structure

Tetrabenazine Chemical Structure

CAS No. : 58-46-8

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Solid + Solvent
10 mM * 1 mL in DMSO
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Solution
10 mM * 1 mL in DMSO USD 55 In-stock
Solid
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100 mg USD 75 In-stock
200 mg USD 120 In-stock
500 mg USD 245 In-stock
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Description

Tetrabenazine (Ro 1-9569) is a reversible inhibitor of the vesicular monoamine transporter VMAT2 with the Kd value of 1.34 nM. Tetrabenazine can be used for research on diseases related to hyperactive movement disorders such as Huntington's disease[1][2][3].

In Vivo

Tetrabenazine (subcutaneous injection, 1-10 mg/kg, once) can reduce the aggressive behavior in a dose-dependent manner and the levels of neurotransmitter molecules NE, DA and 5-HT in adult male mice[1].
Tetrabenazine (intraperitoneal injection, 0-2 mg/kg, once) has selective effects on movement which can significantly attenuate morphine-induced hypermobility but oral tremors and stereotyped behaviors in male ICR mice[2].
Tetrabenazine (intraperitoneal injection, 0.25-2 mg/kg, once a week) increases tremulous jaw movement (TJM) in a dose-dependent manner in adult male Sprague-Dawley rat[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Adult male MAO A KO or wide type mice aged 1-2 months[1]
Dosage: 1-10 mg/kg
Administration: Subcutaneous injection; once
Result: Completely eliminated the aggressive behavior at a concentration of 5 mg/kg and significantly reduced their NE, DA and 5-HT levels.
Animal Model: Male ICR mice (10 weeks old)[2]
Dosage: 0-2 mg/kg
Administration: Intraperitoneal injection; once
Result: Attenuated the subsequent morphine-induced hypermobility after pretreatment with tetrabenazine. Reduced METH-induced increases in locomotion at 1 mg/kg.
Animal Model: Adult male Sprague-Dawley rat weighed 350-450 g[3]
Dosage: 0.25-2 mg/kg
Administration: Intraperitoneal injection; once a week
Result: Induced tremulous jaw movement (TJM) significantly at the concentration of 2 mg/kg and more motor impairments with higher doses such as 3-4 mg/kg.
Clinical Trial
Molecular Weight

317.43

Formula

C19H27NO3

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1[C@@H](CC(C)C)CN2CCC3=CC(OC)=C(OC)C=C3[C@]2([H])C1.[relative stereochemistry]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 33.33 mg/mL (105.00 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1503 mL 15.7515 mL 31.5030 mL
5 mM 0.6301 mL 3.1503 mL 6.3006 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
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Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (7.88 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation

Purity: 98.23%

References

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 3.1503 mL 15.7515 mL 31.5030 mL 78.7575 mL
5 mM 0.6301 mL 3.1503 mL 6.3006 mL 15.7515 mL
10 mM 0.3150 mL 1.5752 mL 3.1503 mL 7.8758 mL
15 mM 0.2100 mL 1.0501 mL 2.1002 mL 5.2505 mL
20 mM 0.1575 mL 0.7876 mL 1.5752 mL 3.9379 mL
25 mM 0.1260 mL 0.6301 mL 1.2601 mL 3.1503 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 1.9689 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 1.3126 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
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Tetrabenazine Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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