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SB 243213 dihydrochloride

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Catalog No. T12859LCas No. 1780372-25-9

SB 243213 dihydrochloride is an orally active, selective, and high-affinity antagonist of the 5-hydroxytryptamine (5-HT)2C receptor, with a pKi of 9.37 and a pKb of 9.8 for the human 5-HT2C receptor.

SB 243213 dihydrochloride

SB 243213 dihydrochloride

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Catalog No. T12859LCas No. 1780372-25-9
SB 243213 dihydrochloride is an orally active, selective, and high-affinity antagonist of the 5-hydroxytryptamine (5-HT)2C receptor, with a pKi of 9.37 and a pKb of 9.8 for the human 5-HT2C receptor.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$15935 days35 days
5 mg$47835 days35 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 243213 dihydrochloride is an orally active, selective, and high-affinity antagonist of the 5-hydroxytryptamine (5-HT)2C receptor, with a pKi of 9.37 and a pKb of 9.8 for the human 5-HT2C receptor.
Targets&IC50
5-HT6 receptor (human):6.5 (pKi), 5-HT1B receptor (human):5.5 (pKi), 5-HT1E receptor (human):<5.4 (pKi), 5-HT1A receptor (human):<5.3 (pKi), 5-HT2A receptor (human):7.01 (pKi), 5-HT7 receptor (human):5.64 (pKi), 5-HT2B receptor (human):7.2 (pKi), 5-HT1D receptor (human):6.32 (pKi), 5-HT2C receptor:9.37 (pKi), 5-HT1F receptor (human):5.35 (pKi)
In vitro
SB 243213 dihydrochloride exhibits low affinity (pKi < 6) for cloned human 5-HT1A, 5-HT1B, 5-HT1E, 5-HT1F, and 5-HT7 receptors, weak affinity (pKi < 6.5) for cloned human 5-HT1D and D3 receptors, and moderate affinity (pKi = 6.7) for the cloned human D2 receptor.
In vivo
SB 243213 dihydrochloride (0.3 mg/kg; p.o.; 1 h pre-test) significantly increases time spent in social interaction. SB 243213 dihydrochloride (0.1-10 mg/kg; p.o.; 1 h pre-test) dose-dependently and significantly increases the amount of time rats spent in social interaction over 15 min under brightly lit conditions and in an unfamiliar test box.
Chemical Properties
Molecular Weight501.33
FormulaC22H21Cl2F3N4O2
Cas No.1780372-25-9
SmilesO=C(N1C2=C(CC1)C=C(C)C(C(F)(F)F)=C2)NC3=CN=C(C=C3)OC4=CC=CN=C4C.Cl.Cl
Relative Density.1.31g/cm3
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

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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
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2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

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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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