Vanoxerine (Synonyms: GBR 12909; I893)

目录号: HY-13217A: FAQs
Data Sheet 产品使用指南

摩尔计算器

Vanoxerine (GBR-12909) 是竞争性的，有效选择性的多巴胺再摄取 (dopamine reuptake) 抑制剂。Vanoxerine (GBR-12909) 与多巴胺转运体 (DAT) 上的靶点结合。

在相同的摩尔浓度下，化合物盐形式与游离形式有相同的生物活性，但盐形式 Vanoxerine dihydrochloride 通常具有更好的水溶性和稳定性。

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Vanoxerine Chemical Structure

CAS No. : 67469-69-6

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Vanoxerine 的其他形式现货产品:

Vanoxerine dihydrochloride

Other Forms of Vanoxerine:

Vanoxerine dihydrochloride In-stock

MCE 顾客使用本产品发表的 5 篇科研文献

: Vanoxerine purchased from MCE. 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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生物活性
纯度 & 产品资料
参考文献

生物活性

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)^[1].

IC₅₀ & Target

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

细胞效力
(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]

体外研究
(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].

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

体内研究
(In Vivo)

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

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

分子量

450.56

Formula

C₂₈H₃₂F₂N₂O

CAS 号

67469-69-6

中文名称

伐诺司林；伐洛司林

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

纯度 & 产品资料

产品使用指南 (1538 KB)

参考文献

[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 相关分类

Neurological Disease

摩尔计算器
稀释计算器

The molarity calculator equation

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

质量		浓度		体积		分子量 *
	=		×		×

The dilution calculator equation

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)	×	体积 _(start)	=	浓度 _(final)	×	体积 _(final)
	×		=		×
C1		V1		C2		V2

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 I893伐诺司林伐洛司林GBR12909GBR-12909I893I 893I-893Dopamine TransporterDATSLC6A3Inhibitorinhibitorinhibit

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营业执照（三证合一）

Vanoxerine (Synonyms: GBR 12909; I893)

Other Forms of Vanoxerine:

MCE 顾客使用本产品发表的 5 篇科研文献

Vanoxerine 相关产品

•同靶点产品:

•同靶点蛋白产品:

生物活性

纯度 & 产品资料

参考文献

Vanoxerine 相关分类

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Vanoxerine (Synonyms: GBR 12909; I893)

Other Forms of Vanoxerine:

Vanoxerine 相关抗体

MCE 顾客使用本产品发表的 5 篇科研文献

Vanoxerine 相关产品

•同靶点产品:

•同靶点蛋白产品:

生物活性

纯度 & 产品资料

参考文献

Vanoxerine 相关抗体:

Vanoxerine 相关分类

摩尔计算器

稀释计算器

The molarity calculator equation

The dilution calculator equation

Keywords:

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