Vanoxerine (Synonyms: GBR 12909; I893)

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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).

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (Vanoxerine dihydrochloride) usually boasts enhanced water solubility and stability.

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

Vanoxerine Chemical Structure

CAS No. : 67469-69-6

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Other In-stock Forms of Vanoxerine:

Vanoxerine dihydrochloride

Other Forms of Vanoxerine:

Vanoxerine dihydrochloride In-stock

5 Publications Citing Use of MCE Vanoxerine

: 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
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References
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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 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	0.11 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	0.79 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	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

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

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

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]

Vanoxerine Related Classifications

Neurological Disease

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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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