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Vapitadine dihydrochloride

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Catalog No. T29096Cas No. 279253-83-7
Alias Vapitadine 2HCl, R-129160 dihydrochloride, R129160 dihydrochloride, R-129160 2HCl, R129160 2HCl, R 129160 2HCl

Vapitadine dihydrochloride(R-129160 2HCl) is a novel, potent, selective and non-sedating compound with inhibitory effects on histamine H1.

Vapitadine dihydrochloride

Vapitadine dihydrochloride

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Purity: 99.30%
Catalog No. T29096Alias Vapitadine 2HCl, R-129160 dihydrochloride, R129160 dihydrochloride, R-129160 2HCl, R129160 2HCl, R 129160 2HClCas No. 279253-83-7
Vapitadine dihydrochloride(R-129160 2HCl) is a novel, potent, selective and non-sedating compound with inhibitory effects on histamine H1.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$258In StockIn Stock
5 mg$642In StockIn Stock
10 mg$913-In Stock
25 mg$1,370-In Stock
50 mg$1,850-In Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products.If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Batch Information

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Purity:99.30%
Appearance:Solid
Color:White to Yellow
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Product Introduction

Vapitadine dihydrochloride AI Summary
Vapitadine dihydrochloride exhibits a range of bioactivities, particularly in histamine-related pathways and allergen-induced reactions. With a moderate LogP value of 1.18, it indicates some level of lipophilicity. It demonstrates high solubility in various buffer solutions across a wide pH range and other media, including water, acidic, and simulated gastrointestinal fluids. The compound shows significant binding affinity for the H1 histamine receptor with a Ki of 19.0 nM. It is effective in inhibiting anaphylactic reactions and histamine-induced shock in rats and guinea pigs, as well as skin reactions caused by various allergens in different animal models. The pKa1 and pKa2 values are 9.88 and 3.0 respectively. Moreover, Vapitadine dihydrochloride exhibits the onset of action within an hour against Ascaris allergen-induced reactions in dogs, maintaining efficacy for 21 hours post-administration. Additionally, it has a calculated partition coefficient (CLogD) value of -1.3. Overall, Vapitadine dihydrochloride shows promising pharmacokinetic and pharmacodynamic properties suited for therapeutic applications in histamine and allergen-induced conditions..
Note: Summary generated by AI. Data source: ChEMBL
Bioactivity
Description
Vapitadine dihydrochloride(R-129160 2HCl) is a novel, potent, selective and non-sedating compound with inhibitory effects on histamine H1.
Targets&IC50
H1 receptor (human):19 nM (Ki)
SynonymsVapitadine 2HCl, R-129160 dihydrochloride, R129160 dihydrochloride, R-129160 2HCl, R129160 2HCl, R 129160 2HCl
Chemical Properties
Molecular Weight369.29
FormulaC17H22Cl2N4O
Cas No.279253-83-7
SmilesO=C(C1=CN=C2N1CCC3=C(C24CCNCC4)C=CC=C3)N.Cl.Cl
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.

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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:
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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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