2. Membrane Transporter/Ion Channel Neuronal Signaling GPCR/G Protein
  3. Monoamine Transporter Dopamine Receptor
  4. Tetrabenazine

Tetrabenazine (Ro 1-9569) is a brain-penetrant and orally active VMAT2-selective ligand with human VMAT2 Ki 100 nM. Tetrabenazine binds VMAT2 to block monoamine uptake into synaptic vesicles, potentiates cytoplasmic monoamine degradation. Tetrabenazine weakly blocks dopamine D2 receptors, and increases dopamine turnover via elevated cerebrospinal fluid homovanillic acid. Tetrabenazine can be used for the research of Huntington’s disease, tardive dyskinesia, and Tourette’s syndrome.

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

Tetrabenazine

Tetrabenazine Chemical Structure

CAS No. : 58-46-8

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
50 mg In-stock
100 mg In-stock
200 mg In-stock
500 mg In-stock
1 g   Get quote  
5 g   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Tetrabenazine:

Tetrabenazine Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Tetrabenazine

View All Dopamine Receptor Isoform Specific Products:

View All Isoforms
Dopamine Receptor D1 Receptor D2 Receptor D3 Receptor D4 Receptor D5 Receptor

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Tetrabenazine (Ro 1-9569) is a brain-penetrant and orally active VMAT2-selective ligand with human VMAT2 Ki 100 nM. Tetrabenazine binds VMAT2 to block monoamine uptake into synaptic vesicles, potentiates cytoplasmic monoamine degradation. Tetrabenazine weakly blocks dopamine D2 receptors, and increases dopamine turnover via elevated cerebrospinal fluid homovanillic acid. Tetrabenazine can be used for the research of Huntington’s disease, tardive dyskinesia, and Tourette’s syndrome[1][2][3].

IC50 & Target

D2 Receptor

~2.1 μM (Ki)

In Vitro

Tetrabenazine reversibly inhibits human VMAT2 with a Ki of ~100 nM, reducing monoamine uptake into synaptic vesicles and depleting presynaptic monoamine stores[1].
Tetrabenazine inhibits dopamine D2 receptors in striatal membranes with a Ki of ~2.1 μM[1].
Tetrabenazine (0.3-10.0 μg/mL; 4 h) releases serotonin from rabbit blood platelets in vitro in a concentration-dependent manner[3].
Tetrabenazine (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 Related Antibodies
In Vivo

Tetrabenazine provides partial neuroprotection in a transgenic HD mouse model of Glutamate-induced striatal neurodegeneration[1].
Tetrabenazine (7 days) causes irreversible locomotor changes and substantia nigra pars compacta neuronal damage in healthy rats[1].
Tetrabenazine (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.

Animal Model: New Zealand White male (~2 kg)[3]
Dosage: 50 mg/kg; 150 mg/kg
Administration: i.v.; daily for 3, 7, 9 days
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.
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
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 : 25 mg/mL (78.76 mM; ultrasonic and warming and heat to 60°C; 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
×
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: ≥ 3.33 mg/mL (10.49 mM); Clear solution

    This protocol yields a clear solution of ≥ 3.33 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (33.3 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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 3.33 mg/mL (10.49 mM); Clear solution

    This protocol yields a clear solution of ≥ 3.33 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (33.3 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.
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: 99.95%

SDS (392 KB)

COA (248 KB) HNMR (274 KB) RP-HPLC (253 KB) MS (68 KB)

Handling Instructions (2659 KB)
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
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

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.

Keywords:

Tetrabenazine58-46-8Ro 1-9569Monoamine TransporterDopamine Receptorsubstantia nigramonoamineTourette’s syndromerabbit blood plateletscerebrospinal fluid homovanillic acidstriatal membraneshuman dopamine D2 receptortransgenic HD mouse modelVMAT2Huntington’s diseaseInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Tetrabenazine
Cat. No.:
HY-B0590
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

English - EN (392 KB) Français - FR (392 KB) Deutsch - DE (392 KB) Norwegian - NO (392 KB) Español - ES (392 KB) Swedish - SV (392 KB) Italian - IT (392 KB) Korean - KR (392 KB) Portuguese - PT (392 KB)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.