Vanoxerine (Synonyms: GBR 12909; I893)

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

製品番号: HY-13217A 純度: 98.06%: Data Sheet SDS COA 取扱説明書
FAQs
Technical Support

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).

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

CAS 番号 : 67469-69-6

容量	価格（税別）	在庫状況	数量
Oil + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 102	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 102	在庫あり	Estimated Time of Arrival: December 31
Oil
10 mg	$93	在庫あり	Estimated Time of Arrival: December 31
25 mg	$186	在庫あり	Estimated Time of Arrival: December 31
50 mg	$280	在庫あり	Estimated Time of Arrival: December 31
100 mg	$420	在庫あり	Estimated Time of Arrival: December 31
200 mg		お問い合わせ
500 mg		お問い合わせ

or バルクお問い合わせ

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 8 publication(s) in Google Scholar

Other Forms of Vanoxerine:

Vanoxerine dihydrochloride 在庫あり

顧客検証

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.

おすすめ

•関連スクリーニングライブラリ:

•関連小分子:

•関連タンパク質:

生物活性
純度とドキュメンテーション
参考文献
カスタマーレビュー

製品説明

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]

体外実験

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.

体内実験

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.

臨床実験

分子量

450.56

分子式

C₂₈H₃₂F₂N₂O

CAS 番号

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

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

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

溶剤 & 溶解度

体外:

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)

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

体内:

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.

純度とドキュメンテーション

純度: 98.06%

Select Batch:

データシート (271 KB) SDS (254 KB)

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

取扱説明書 (2659 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]

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

Molarity Calculator
Dilution Calculator

The molarity calculator equation

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

質量		濃度		体積		分子量 *
	=		×		×

The dilution calculator equation

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

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）	×	体積 _（開始）	=	濃度 _（終了）	×	体積 _（終了）
	×		=		×
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 I893GBR12909GBR-12909I893I 893I-893Dopamine TransporterDATSLC6A3Inhibitorinhibitorinhibit

最近チェックした製品:

製品名

カスタマ需要量 *

お名前 *

タイトル

メールアドレス *

電話番号 *

デパートメント

組纖名 *

市区町村

都道府県

国或いは地域 *

必ず会社名を記載ください。個人への返信は行いません。

備考

製品名

Lot #

お名前 *

メールアドレス *

電話番号 *

部門 *

組纖名 *

国或いは地域 *

備考

お名前
メール *

	Sorry, but the email address you supplied was invalid.

Vanoxerine (Synonyms: GBR 12909; I893)

カスタマーレビュー

Other Forms of Vanoxerine:

Vanoxerine 関連抗体

顧客検証

おすすめ

•関連スクリーニングライブラリ:

•関連小分子:

•関連タンパク質:

生物活性

純度とドキュメンテーション

参考文献

カスタマーレビュー

Vanoxerine 関連抗体

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Vanoxerine Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

Keywords:

最近チェックした製品:

カスタマーレビュー

Request for HNMR Report

Request for HNMR Report