Cat. No.: HY-13217A

Vanoxerine

(Synonyms: GBR 12909; I893)

11 Cited Publications

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Based on 11 publication(s) in Google Scholar

Vanoxerine (GBR-12909) is a competitive, potent, and highly selective dopamine reuptake inhibitor (K_i=1 nM). Vanoxerine (GBR-12909) binds to the target site on the dopamine transporter (DAT).

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Pureté: 98.06%
CAS No.: 67469-69-6
Formule: C₂₈H₃₂F₂N₂O
Masse moléculaire:450.56

Stockage:

Pure form -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Vanoxerine Chemical Structure

CAS No.: 67469-69-6

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (11)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

Ki: 1 nM (dopamine reuptake)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	0.04 μM Compound: GBR12909	Inhibition of re-uptake of [3H]-DA at human DAT expressed in HEK293 cells by liquid scintillation counting Inhibition of re-uptake of [3H]-DA at human DAT expressed in HEK293 cells by liquid scintillation counting	[PMID: 28807575]
HEK293	IC₅₀	0.043 μM Compound: GBR12909	Inhibition of [3H]-5-dopamine reuptake in human DAT expressed in HEK293 cells by microbeta liquid scintillation counting method Inhibition of [3H]-5-dopamine reuptake in human DAT expressed in HEK293 cells by microbeta liquid scintillation counting method	[PMID: 28274674]
HEK293	IC₅₀	0.11 μM Compound: GBR12909	Inhibition of [3H]-5-norepinephrine reuptake in human NET expressed in HEK293 cells by microbeta liquid scintillation counting method Inhibition of [3H]-5-norepinephrine reuptake in human NET expressed in HEK293 cells by microbeta liquid scintillation counting method	[PMID: 28274674]
HEK293	IC₅₀	0.11 μM Compound: GBR12909	Inhibition of re-uptake of [3H]-NE at human NET expressed in HEK293 cells by liquid scintillation counting Inhibition of re-uptake of [3H]-NE at human NET expressed in HEK293 cells by liquid scintillation counting	[PMID: 28807575]
HEK293	IC₅₀	0.79 μM Compound: GBR12909	Inhibition of the Norepinephrine transporter (NET, SLC6A2) as assessed by GPCR-mediated changes in cell morphology using the impedance-based transporter activity through receptor activation (TRACT) assay in HEK-293 JumpIN-SLC6A2 cells Inhibition of the Norepinephrine transporter (NET, SLC6A2) as assessed by GPCR-mediated changes in cell morphology using the impedance-based transporter activity through receptor activation (TRACT) assay in HEK-293 JumpIN-SLC6A2 cells	[PMID: 34112854]
HEK293	IC₅₀	0.79 μM Compound: GBR12909	Inhibition of the Norepinephrine transporter (NET, SLC6A2) as assessed by GPCR-mediated changes in cell morphology using the impedance-based transporter activity through receptor activation (TRACT) assay in HEK-293 JumpIN-SLC6A2 cells (PubChem AID: 174586 Inhibition of the Norepinephrine transporter (NET, SLC6A2) as assessed by GPCR-mediated changes in cell morphology using the impedance-based transporter activity through receptor activation (TRACT) assay in HEK-293 JumpIN-SLC6A2 cells (PubChem AID: 174586	[PMID: 34112854]
HEK293	IC₅₀	1460 nM Compound: GBR12909	Inhibition of human NET expressed in HEK293 cells at incubated for 15 mins by neurotransmitter reuptake assay Inhibition of human NET expressed in HEK293 cells at incubated for 15 mins by neurotransmitter reuptake assay	[PMID: 25221656]
HEK293	IC₅₀	190 nM Compound: GBR12909	Inhibition of human DAT expressed in HEK293 cells at incubated for 15 mins by neurotransmitter reuptake assay Inhibition of human DAT expressed in HEK293 cells at incubated for 15 mins by neurotransmitter reuptake assay	[PMID: 25221656]
HEK293	IC₅₀	26 nM Compound: GBR-12909	Affinity was evaluated using [3H]DA (radioligand) on Cloned human Dopamine transporter expressed in HEK cells Affinity was evaluated using [3H]DA (radioligand) on Cloned human Dopamine transporter expressed in HEK cells	[PMID: 9703474]
HEK293	IC₅₀	3840 nM Compound: GBR12909	Inhibition of human SERT expressed in HEK293 cells at incubated for 15 mins by neurotransmitter reuptake assay Inhibition of human SERT expressed in HEK293 cells at incubated for 15 mins by neurotransmitter reuptake assay	[PMID: 25221656]
HEK293	IC₅₀	43 nM Compound: GBR-12909	Affinity was evaluated using [3H]WIN-35428 (radioligand) on Cloned human Dopamine transporter expressed in HEK cells Affinity was evaluated using [3H]WIN-35428 (radioligand) on Cloned human Dopamine transporter expressed in HEK cells	[PMID: 9703474]
HEK293	IC₅₀	741 nM Compound: GBR-12909	Affinity was evaluated using [3H]citalopram (radioligand) on human serotonin transporter expressed in HEK cells Affinity was evaluated using [3H]citalopram (radioligand) on human serotonin transporter expressed in HEK cells	[PMID: 9703474]
Ventricular myocyte	IC₅₀	0.32 μM Compound: Vanoredxine (GBR-12909)	Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes	[PMID: 22761000]

In Vitro

Vanoxerine (GBR-12909) inhibits the uptake of dopamlne (DA), with an IC₅₀ in the low nanomolar range, and is several-fold less potent as inhibitors of the uptake of noradrenaline and 5-HT^[2].
Vanoxerine (GBR-12909) is also an oral, mixed ion channel blocker with IKr, INa, and L-type calcium channel activity^[3].

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

In Vivo

Vanoxerine (GBR-12909) (2.5-20 mg/kg; i.p.) significantly increases the ambulatory activity^[3].

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

Animal Model:

Male mice(ddY strain at 6 weeks of age)^[3]
Dosage:

2.5, 5, 10, 20 mg/kg
Administration:

Intraperitoneal injection
Result:

The ambulatory activity of mice increased in a dose-dependent manner, with a maximal increase at 30 min after the administration.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 67469-69-6
Appearance Oil
Masse moléculaire 450.56
Formule C₂₈H₃₂F₂N₂O
Color Colorless to light yellow
SMILES

FC1=CC=C(C(C2=CC=C(F)C=C2)OCCN3CCN(CCCC4=CC=CC=C4)CC3)C=C1
Synonyms

GBR 12909; I893
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Pure form	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (11)

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Journal Impact Factor

Nature

Dopamine reuptake and inhibitory mechanisms in human dopamine transporter. [Abstract]

2024 Aug;632(8025):686-694. PMID: 39112701

Vanoxerine purchased from MedChemExpress. Usage Cited in: Nature. 2024 Aug;632(8025):686-694. [Abstract]

Concentration–inhibition curves of [3H]dopamine uptake by wild-type and indicated mutants of DAT with specified concentrations of GBR12909 (Vanoxerine dihydrochloride) in the range of 1 pM to 10 μM.
Cell

Unveiling conformation-selective regulation of the norepinephrine transporter. [Abstract]

2025 Nov 26;188(24):6861-6872.e14. PMID: 41138730
Nat Commun

Targeting dopamine transporter for treating social transmission of depression-like behaviors in male mice. [Abstract]

2026 Jun 16. PMID: 42303982
Neuron

Propofol exerts anti-anhedonia effects via inhibiting the dopamine transporter. [Abstract]

2023 May 17;111(10):1626-1636.e6. PMID: 36917979
Cell Discov

TGM2-mediated serotonylation of GPX4 confers ferroptosis resistance to promote gastric tumorigenesis. [Abstract]

2026 Apr 28;12(1):30. PMID: 42049702
Transl Psychiatry

MicroRNA-132/212 negatively modulates opioid reward by targeting dopamine transporter in the ventral tegmental area. [Abstract]

2026 Feb 25;16(1):152. PMID: 41741420
Structure

2026 Jun 8.
Front Cell Neurosci

Differential Regulation of Adhesion and Phagocytosis of Resting and Activated Microglia by Dopamine. [Abstract]

2018 Sep 11:12:309. PMID: 30254570

Vanoxerine purchased from MedChemExpress. Usage Cited in: Front Cell Neurosci. 2018 Sep 11:12:309. [Abstract]

p38MAPK activation by dopamine (DA) can be inhibited by selective DAT blockers (Benztropine and Vanoxerine; 2 μM each) and PMAT blocker (Decynium; 2 μM). Combination of DAT and PMAT blockers further inhibits the activation of p38MAPK.
Biochem Biophys Res Commun

PGC-1α regulate critical period plasticity via gene × environment interaction in the developmental trajectory to schizophrenia. [Abstract]

2020 May 14;525(4):989-996. PMID: 32173526
bioRxiv

In vivo multiplex imaging of dynamic neurochemical networks with designed far-red dopamine sensors. [Abstract]

2024 Dec 23:2024.12.22.629999. PMID: 39763912
University of Groningen

2016 Jun 1.

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (221.95 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2195 mL

11.0973 mL

22.1946 mL

5 mM

0.4439 mL

2.2195 mL

4.4389 mL

10 mM

0.2219 mL

1.1097 mL

2.2195 mL

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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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 90% Corn Oil

Solubility: ≥ 5 mg/mL (11.10 mM); Clear solution

This protocol yields a clear solution of ≥ 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 (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (271 KB)
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Rothman RB, et al. Dopamine transport inhibitors based on GBR12909 and benztropine as potential medications to treat cocaine addiction. Biochem Pharmacol. 2008 Jan 1;75(1):2-16. [Content Brief]

[2]. Andersen PH. The dopamine inhibitor GBR 12909: selectivity and molecular mechanism of action. Eur J Pharmacol. [Content Brief]

[3]. Hirate K, et al. Characteristics of the ambulation-increasing effect of GBR-12909, a selective dopamine uptakeinhibitor, in mice. Jpn J Pharmacol. 1991 Apr;55(4):501-11. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.2195 mL	11.0973 mL	22.1946 mL	55.4865 mL
	5 mM	0.4439 mL	2.2195 mL	4.4389 mL	11.0973 mL
	10 mM	0.2219 mL	1.1097 mL	2.2195 mL	5.5487 mL
	15 mM	0.1480 mL	0.7398 mL	1.4796 mL	3.6991 mL
	20 mM	0.1110 mL	0.5549 mL	1.1097 mL	2.7743 mL
	25 mM	0.0888 mL	0.4439 mL	0.8878 mL	2.2195 mL
	30 mM	0.0740 mL	0.3699 mL	0.7398 mL	1.8496 mL
	40 mM	0.0555 mL	0.2774 mL	0.5549 mL	1.3872 mL
	50 mM	0.0444 mL	0.2219 mL	0.4439 mL	1.1097 mL
	60 mM	0.0370 mL	0.1850 mL	0.3699 mL	0.9248 mL
	80 mM	0.0277 mL	0.1387 mL	0.2774 mL	0.6936 mL
	100 mM	0.0222 mL	0.1110 mL	0.2219 mL	0.5549 mL

Keywords

Vanoxerine

11 Cited Publications

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Vanoxerine

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Membrane Protein-targeted Compound Library

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Publications Citing Use of MedChemExpress (MCE) Vanoxerine

Activité biologique

Chemical Information

Publications (11)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Vanoxerine

Neuronal Signaling Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Human Metabolite Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Publications Citing Use of MedChemExpress (MCE) Vanoxerine

Activité biologique

Chemical Information

Publications (11)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Vanoxerine Related Classifications

HY-13217A Related Classifications