Size | Price | Stock | Qty |
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50mg |
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100mg |
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250mg |
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500mg |
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Other Sizes |
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Vanoxerine dihydrochloride (GBR-12909; I-893) is a novel, potent, competitive and highly selective dopamine ruptake inhibitor (Ki=1 nM) with the potential for the treatment of atrial fibrillation. GBR 12909 effectively inhibits dopamine uptake in vivo. GBR-12909 binds to the target site on the dopamine transporter (DAT) ~ 50 times more strongly than cocaine, but simultaneously inhibits the release of dopamine. This combined effect only slightly elevates dopamine levels, giving vanoxerine only mild stimulant effects.[2] Vanoxerine has also been observed to be a potent blocker of the IKr (hERG) channel. GBR-12909 also binds with nanomolar affinity to the serotonin transporter.
ln Vitro |
Vanoxerine diHClide (GBR-12909 diHClide) is a low-fold effective supplement of norepinephrine and serotonin that suppresses the nutrient dopamine (DA) with an IC50 in the low nanomolar range [2]. Another wall mixed ion channel blocker having IKr, INa, and L-type calcium channel action is -12909 dihydrochloride [3].
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Animal Protocol |
Animal/Disease Models: Male mice (6 weeks old ddY strain) [3]
Doses: 2.5, 5, 10, 20 mg/kg Varnosline hydrochloride (2.5-20 mg/kg; intraperitoneal (ip) injection) Dramatically increases walking activity [ 3]. Route of Administration: intraperitoneal (ip) injection. Experimental Results: The walking activity of mice increased in a dose-dependent manner, with the maximum increase 30 minutes after administration. |
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.
[2]. 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. [3]. Andersen PH. The dopamine inhibitor GBR 12909: selectivity and molecular mechanism of action. Eur J Pharmacol. |
Molecular Formula |
C28H34CL2F2N2O
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Molecular Weight |
523.4852
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CAS # |
67469-78-7
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Related CAS # |
Vanoxerine;67469-69-6
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
FC1=CC=C(C(C2=CC=C(F)C=C2)OCCN3CCN(CCCC4=CC=CC=C4)CC3)C=C1.[H]Cl.[H]Cl
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InChi Key |
MIBSKSYCRFWIRU-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C28H32F2N2O.2ClH/c29-26-12-8-24(9-13-26)28(25-10-14-27(30)15-11-25)33-22-21-32-19-17-31(18-20-32)16-4-7-23-5-2-1-3-6-23/h1-3,5-6,8-15,28H,4,7,16-22H22*1H
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Chemical Name |
1-(2-[bis(4-Fluorophenyl)methoxy]ethyl)-4-(3-phenylpropyl)piperazine dihydrochloride
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Synonyms |
Vanoxerine DiHCl GBR 12909 GBR-12909 GBR12909.
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO : ~9.4 mg/mL (~17.96 mM)
H2O : ~1 mg/mL (~1.91 mM) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.97 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (3.97 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (3.97 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.9103 mL | 9.5513 mL | 19.1026 mL | |
5 mM | 0.3821 mL | 1.9103 mL | 3.8205 mL | |
10 mM | 0.1910 mL | 0.9551 mL | 1.9103 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.