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(±)-Tazifylline

🥰Excellent
Catalog No. T10000Cas No. 79712-55-3

(±)-Tazifylline is a selective and long-acting antagonist of histamine H1 receptor. Tazifylline shows much lower affinity for H2 receptors, α- and β-adrenoceptors, 5-hydroxytryptamine and muscarinic receptor subtypes.

(±)-Tazifylline

(±)-Tazifylline

🥰Excellent
Purity: 99.54%
Catalog No. T10000Cas No. 79712-55-3
(±)-Tazifylline is a selective and long-acting antagonist of histamine H1 receptor. Tazifylline shows much lower affinity for H2 receptors, α- and β-adrenoceptors, 5-hydroxytryptamine and muscarinic receptor subtypes.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$151In StockIn Stock
5 mg$298In StockIn Stock
10 mg$433In StockIn Stock
25 mg$678In StockIn Stock
50 mg$912In StockIn Stock
100 mg$1,180In StockIn Stock
1 mL x 10 mM (in DMSO)$389In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.54%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
(±)-Tazifylline is a selective and long-acting antagonist of histamine H1 receptor. Tazifylline shows much lower affinity for H2 receptors, α- and β-adrenoceptors, 5-hydroxytryptamine and muscarinic receptor subtypes.
In vitro
Tazifylline potently inhibits histamine H1-receptor-induced contractions in isolated guinea pig ilea and demonstrates high affinity in radioligand binding studies[1].
In vivo
In anesthetized guinea pigs, Tazifylline causes an inhibition in histamine-induced bronchoconstriction and protects conscious animals from the lethal effect of large doses of the amine. In conscious rats, Tazifylline reduces the inflammatory effects of intradermal histamine. In conscious dogs, Tazifylline(orally) causes inhibition in histamine-induced skin inflammation for long periods of time, and in anesthetized animals attenuated that portion of the histamine-evoked hypotension attributable to stimulation of H1 receptors. Large oral doses of Tazifylline do not reduce spontaneous locomotor activity in mice, nor do they produce overt symptoms of behavioral depression in conscious rats[1].
Chemical Properties
Molecular Weight472.6
FormulaC23H32N6O3S
Cas No.79712-55-3
SmilesC(C(CN1CCN(CCCSC2=CC=CC=C2)CC1)O)N3C4=C(N=C3)N(C)C(=O)N(C)C4=O
Relative Density.1.34g/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: 45 mg/mL (95.22 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.1160 mL10.5798 mL21.1595 mL105.7977 mL
5 mM0.4232 mL2.1160 mL4.2319 mL21.1595 mL
10 mM0.2116 mL1.0580 mL2.1160 mL10.5798 mL
20 mM0.1058 mL0.5290 mL1.0580 mL5.2899 mL
50 mM0.0423 mL0.2116 mL0.4232 mL2.1160 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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