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Niaprazine

Catalog No. T36949 Copy Product Info
Purity: 99.56%
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Niaprazine is a histamine H1-receptor antagonist exhibiting significant sedative properties.

Niaprazine

Copy Product Info
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Catalog No. T36949

Niaprazine is a histamine H1-receptor antagonist exhibiting significant sedative properties.

Niaprazine
Cas No. 27367-90-4
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Pack SizePriceUSA StockGlobal StockQuantity
5 mg$30In StockIn Stock
10 mg$48In StockIn Stock
25 mg$96In StockIn Stock
50 mg$155In StockIn Stock
100 mg$228In StockIn Stock
200 mg$328In StockIn Stock
1 mL x 10 mM (in DMSO)$32In StockIn Stock
In stock · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)
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Purity:99.56%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
Niaprazine is a histamine H1-receptor antagonist exhibiting significant sedative properties.
Targets&IC50
5-HT2:25 nM(Ki), α1-adrenoceptor:77 nM(Ki)
In vitro
Niaprazine demonstrates a low affinity for the vesicular monoamine transporter as well as D2, α2, β, H1, and mAch receptors. Notably, the (+)stereoisomer of Niaprazine shows a significantly higher affinity for α1 (Ki = 77 nM) and 5-HT2 (Ki = 25 nM) binding sites, whereas it is poorly recognized by 5-HT1A and 5-HT1B binding sites[2].
In vivo
Niaprazine (60 mg/kg; i.p.; once) treatment increases rat brain 5-hydroxyindole acetic acid (5-HIAA) concentrations 30 minutes post-treatment but reduces them 3-8 hours after treatment. Niaprazine also temporarily depletes rat brain noradrenaline (NA) and dopamine (DA) levels[3]. Animal Model: Male Sprague-Dawley rats (150-200 g)[3].
Chemical Properties
Molecular Weight356.44
FormulaC20H25FN4O
Cas No.27367-90-4
SmilesCC(CCN1CCN(CC1)c1ccc(F)cc1)NC(=O)c1cccnc1
Relative Density.1.165 g/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.
Solubility Information
DMSO: 100 mg/mL (280.55 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween-80+45% Saline: 1 mg/mL (2.81 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.8055 mL14.0276 mL28.0552 mL140.2761 mL
5 mM0.5611 mL2.8055 mL5.6110 mL28.0552 mL
10 mM0.2806 mL1.4028 mL2.8055 mL14.0276 mL
20 mM0.1403 mL0.7014 mL1.4028 mL7.0138 mL
50 mM0.0561 mL0.2806 mL0.5611 mL2.8055 mL
100 mM0.0281 mL0.1403 mL0.2806 mL1.4028 mL
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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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

You can also refer to dose conversion for different animals. More Dose Conversion

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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