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Transcainide

🥰Excellent
Catalog No. T26287Cas No. 88296-62-2
Alias R-54718, R54718, R 54718

Transcainide(R 54718), a new lidocaine analog, is an orally active antiarrhythmic agent.Transcainide blocks the open state of BTX-activated sodium channels in bovine heart and rat skeletal muscle.

Transcainide

Transcainide

🥰Excellent
Purity: 99.81%
Catalog No. T26287Alias R-54718, R54718, R 54718Cas No. 88296-62-2
Transcainide(R 54718), a new lidocaine analog, is an orally active antiarrhythmic agent.Transcainide blocks the open state of BTX-activated sodium channels in bovine heart and rat skeletal muscle.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$161In StockIn Stock
5 mg$398In StockIn Stock
10 mg$566In StockIn Stock
25 mg$833In 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:99.81%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
Transcainide(R 54718), a new lidocaine analog, is an orally active antiarrhythmic agent.Transcainide blocks the open state of BTX-activated sodium channels in bovine heart and rat skeletal muscle.
In vitro
Transcainide (IC50=0.3 μM) inhibited equilibrium [3H]batrachotoxinin binding to sodium channels present on freshly isolated rat cardiac myocytes. Scatchard analysis of [3H]batrachotoxinin binding showed that Transcainide both reduced maximal binding and altered the KD for [3H]batrachotoxinin binding, indicating noncompetitive, allosteric inhibition. Inhibition by Transcainide of [3H]batrachotoxinin binding was reversible within 60 min. Transcainide had little effect on the k-1 of [3H]batrachotoxinin even at concentrations 1000-fold greater than its IC50, indicating a low affinity of Transcainide for activated channels. However, Transcainidee decreased the k + 1 of [3H]batrachotoxinin at a concentration very close to its IC50 concentration for inhibiting equilibrium [3H] batrachotoxin binding. The results are discussed in terms of a model in which Transcainide inhibits [3H] batrachotoxin binding by binding specifically to and stabilizing a nonactivated state of the cardiac sodium channel.[1]
Reduction of sodium current by Transcainide was concentration-dependent, with an ED50 of approximately 0.5 μM (n = 9).[2]
SynonymsR-54718, R54718, R 54718
Chemical Properties
Molecular Weight373.53
FormulaC22H35N3O2
Cas No.88296-62-2
SmilesC(NC1=C(C)C=CC=C1C)(=O)C2(N(C)C)CCN(CC2)[C@H]3[C@H](O)CCCC3
Relative Density.1.13g/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: 3.74 mg/mL (10.01 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.6772 mL13.3858 mL26.7716 mL133.8581 mL
5 mM0.5354 mL2.6772 mL5.3543 mL26.7716 mL
10 mM0.2677 mL1.3386 mL2.6772 mL13.3858 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:
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2 Enter the in vivo formulation:
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