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SB-200646A

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Catalog No. T22423Cas No. 143797-62-0

SB-200646A is an orally active, selective antagonist of 5-HT2B/2C over 5-HT2A receptor with pKi of 7.5, 6.9 and 5.2 for 5-HT2B, 5-HT2C and 5-HT2A, respectively. SB-200646A exerts anxiolytic and electrophysiological properties in vivo.

SB-200646A

SB-200646A

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Catalog No. T22423Cas No. 143797-62-0
SB-200646A is an orally active, selective antagonist of 5-HT2B/2C over 5-HT2A receptor with pKi of 7.5, 6.9 and 5.2 for 5-HT2B, 5-HT2C and 5-HT2A, respectively. SB-200646A exerts anxiolytic and electrophysiological properties in vivo.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
2 mg$355 days5 days
1 mL x 10 mM (in DMSO)$765 days5 days
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Product Introduction

Bioactivity
Description
SB-200646A is an orally active, selective antagonist of 5-HT2B/2C over 5-HT2A receptor with pKi of 7.5, 6.9 and 5.2 for 5-HT2B, 5-HT2C and 5-HT2A, respectively. SB-200646A exerts anxiolytic and electrophysiological properties in vivo.
Targets&IC50
5-HT2A receptor:5.2 (pKi), 5-HT2C receptor:6.9 (pKi), 5-HT2B receptor:7.5 (pKi)
In vitro
SB200646A (4 μM) eliminates the increase in miniature inhibitory postsynaptic current (mIPSC) frequency induced by ethanol, without affecting the basal mIPSC frequency.
In vivo
SB-200646A (20 mg/kg; intravenous injection; daily; for 21 days; male albino Sprague-Dawley rats) significantly decreases the number of spontaneously active ventral tegmental area (VTA) dopaminergic neurons. Intravenous administration of 4-16 mg/kg of SB-200646A significantly increases the firing rate and percentage of events as bursts in spontaneously active VTA dopaminergic neurons and increases the percentage of events as burst in substantia nigra pars compacta (SNC) dopaminergic neurons[1].
Chemical Properties
Molecular Weight302.76
FormulaC15H15ClN4O
Cas No.143797-62-0
SmilesCl.Cn1ccc2cc(NC(=O)Nc3cccnc3)ccc12
Relative Density.no data available
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 225 mg/mL (743.16 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM3.3029 mL16.5147 mL33.0295 mL165.1473 mL
5 mM0.6606 mL3.3029 mL6.6059 mL33.0295 mL
10 mM0.3303 mL1.6515 mL3.3029 mL16.5147 mL
20 mM0.1651 mL0.8257 mL1.6515 mL8.2574 mL
50 mM0.0661 mL0.3303 mL0.6606 mL3.3029 mL
100 mM0.0330 mL0.1651 mL0.3303 mL1.6515 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

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