Vanoxerine
Based on 11 publication(s) in Google Scholar
Vanoxerine (GBR-12909) is a competitive, potent, and highly selective dopamine reuptake inhibitor (Ki=1 nM). Vanoxerine (GBR-12909) binds to the target site on the dopamine transporter (DAT).
For research use only. We do not sell to patients.
- Purity: 98.06%
- CAS No.: 67469-69-6
- Formula: C28H32F2N2O
- Molecular Weight:450.56
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Storage:Pure form -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Vanoxerine
More- Nature. 2024 Aug;632(8025):686-694. [Abstract]
- Cell. 2025 Nov 26;188(24):6861-6872.e14. [Abstract]
- Nat Commun. 2026 Jun 16. [Abstract]
- Neuron. 2023 May 17;111(10):1626-1636.e6. [Abstract]
- Cell Discov. 2026 Apr 28;12(1):30. [Abstract]
- Transl Psychiatry. 2026 Feb 25;16(1):152. [Abstract]
- Structure. 2026 Jun 8.
- Front Cell Neurosci. 2018 Sep 11:12:309. [Abstract]
- Biochem Biophys Res Commun. 2020 May 14;525(4):989-996. [Abstract]
- bioRxiv. 2024 Dec 23:2024.12.22.629999. [Abstract]
- University of Groningen. 2016 Jun 1.
Customer Validation & Images
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Others
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Biological Activity
Ki: 1 nM (dopamine reuptake)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
0.04 μM
Compound: GBR12909
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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
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[PMID: 28807575] |
| HEK293 | IC50 |
0.043 μM
Compound: GBR12909
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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
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[PMID: 28274674] |
| HEK293 | IC50 |
0.11 μM
Compound: GBR12909
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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
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[PMID: 28274674] |
| HEK293 | IC50 |
0.11 μM
Compound: GBR12909
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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
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[PMID: 28807575] |
| HEK293 | IC50 |
0.79 μM
Compound: GBR12909
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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
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[PMID: 34112854] |
| HEK293 | IC50 |
0.79 μM
Compound: GBR12909
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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
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[PMID: 34112854] |
| HEK293 | IC50 |
1460 nM
Compound: GBR12909
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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
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[PMID: 25221656] |
| HEK293 | IC50 |
190 nM
Compound: GBR12909
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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
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[PMID: 25221656] |
| HEK293 | IC50 |
26 nM
Compound: GBR-12909
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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
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[PMID: 9703474] |
| HEK293 | IC50 |
3840 nM
Compound: GBR12909
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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
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[PMID: 25221656] |
| HEK293 | IC50 |
43 nM
Compound: GBR-12909
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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
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[PMID: 9703474] |
| HEK293 | IC50 |
741 nM
Compound: GBR-12909
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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
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[PMID: 9703474] |
| Ventricular myocyte | IC50 |
0.32 μM
Compound: Vanoredxine (GBR-12909)
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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
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[PMID: 22761000] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male mice(ddY strain at 6 weeks of age)[3]
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Dosage:2.5, 5, 10, 20 mg/kg
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Administration:Intraperitoneal injection
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Result:The ambulatory activity of mice increased in a dose-dependent manner, with a maximal increase at 30 min after the administration.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 67469-69-6
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Appearance Oil
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Molecular Weight 450.56
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Formula C28H32F2N2O
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Color Colorless to light yellow
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SMILES
FC1=CC=C(C(C2=CC=C(F)C=C2)OCCN3CCN(CCCC4=CC=CC=C4)CC3)C=C1
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Synonyms
GBR 12909; I893
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
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
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Most Recent
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Nature
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.
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Cell
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
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 -
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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.
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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 -
Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
Purity & Documentation
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Data Sheet (271 KB)
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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)
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Handling Instructions (2659 KB)
References
[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]
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, 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 |
Vanoxerine Related Classifications
HY-13217A Related Classifications
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