Vanoxerine (Synonyms: GBR 12909; I893)

Name: Vanoxerine
Brand: MedChemExpress
SKU: HY-13217A
Rating: 5.0 (8 reviews)

Cat. No.: HY-13217A Purity: 98.06%: Data Sheet
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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).

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

CAS No. : 67469-69-6

Size	Stock	Quantity
Oil + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Oil
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Customer Review

Based on 8 publication(s) in Google Scholar

Other Forms of Vanoxerine:

Vanoxerine dihydrochloride In-stock

8 Publications Citing Use of MCE Vanoxerine

Others

: 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.

: 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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Biological Activity
Purity & Documentation
References
Customer Review

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 (PubChem AID: 1745860) 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: 1745860)	[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.

Clinical Trial

Molecular Weight

450.56

Formula

C₂₈H₃₂F₂N₂O

CAS No.

67469-69-6

Appearance

Oil

Color

Colorless to light yellow

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

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, 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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 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

mg/kg

Animal weight
(per animal)

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: 98.06%

Select Batch:

Data Sheet (271 KB) SDS (254 KB)

COA (244 KB) HNMR (141 KB) RP-HPLC (169 KB) LCMS (108 KB)

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

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

Neurological Disease

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:

Vanoxerine67469-69-6GBR 12909 I893GBR12909GBR-12909I893I 893I-893Dopamine TransporterDATSLC6A3Inhibitorinhibitorinhibit

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Vanoxerine (Synonyms: GBR 12909; I893)

Customer Review

Other Forms of Vanoxerine:

Vanoxerine Related Antibodies

8 Publications Citing Use of MCE Vanoxerine

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity

Purity & Documentation

References

Customer Review

Vanoxerine Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Vanoxerine Related Classifications

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