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Samelisant

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Catalog No. T9770Cas No. 1394808-82-2
Alias SUVN-G3031

Samelisant (SUVN-G3031) is a selective and inverse agonist of H3 receptor with Kis of 8.7 nM and 9.8 nM for human and rat. Samelisant has anticataplectic effects and can be used in studies about narcolepsy.

Samelisant

Samelisant

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Purity: 99.59%
Catalog No. T9770Alias SUVN-G3031Cas No. 1394808-82-2
Samelisant (SUVN-G3031) is a selective and inverse agonist of H3 receptor with Kis of 8.7 nM and 9.8 nM for human and rat. Samelisant has anticataplectic effects and can be used in studies about narcolepsy.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$113-In Stock
2 mg$169-In Stock
5 mg$289-In Stock
10 mg$463-In Stock
25 mg$763-In Stock
50 mg$1,070-In Stock
100 mg$1,430-In Stock
500 mg$2,890-In Stock
1 mL x 10 mM (in DMSO)$297-In Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.59%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
Samelisant (SUVN-G3031) is a selective and inverse agonist of H3 receptor with Kis of 8.7 nM and 9.8 nM for human and rat. Samelisant has anticataplectic effects and can be used in studies about narcolepsy.
In vitro
Samelisant (1, 10, and 100 nM) increases the pEC50 from 8.5 to 8.2, 7.3, and 6.2 for human H3 receptor and from 8.2 to 7.9, 7.4, and 6.4 for rat H3 receptor, respectively. Samelisant modulates dopamine and norepinephrine levels in the cerebral cortex. Samelisant reversibly binds to the orthosteric site with Kbs of 1.3 nM and 1.1 nM[1].
In vivo
In orexin knockout mice subjected to sleep EEG, Samelisant (10 and 30 mg/kg; p.o.) significantly increases wakefulness and concomitantly decreases NREM sleep. Samelisant significantly decreases direct REM sleep onset episodes and dose-dependently increases the level of tele-methylhistamine[1].
SynonymsSUVN-G3031
Chemical Properties
Molecular Weight373.49
FormulaC21H31N3O3
Cas No.1394808-82-2
SmilesO(C1CCN(CC1)C2CCC2)C3=CC=C(NC(CN4CCOCC4)=O)C=C3
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: 50 mg/mL (133.87 mM), Sonication and heating to 60℃ are recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.6774 mL13.3872 mL26.7745 mL133.8724 mL
5 mM0.5355 mL2.6774 mL5.3549 mL26.7745 mL
10 mM0.2677 mL1.3387 mL2.6774 mL13.3872 mL
20 mM0.1339 mL0.6694 mL1.3387 mL6.6936 mL
50 mM0.0535 mL0.2677 mL0.5355 mL2.6774 mL
100 mM0.0268 mL0.1339 mL0.2677 mL1.3387 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
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μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

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