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Transcainide

Transcainide
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Purity:100%
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Transcainide

Catalog No. T26287Cas 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.
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Pack SizePriceAvailabilityQuantity
1 mg$268In Stock
5 mg$663In Stock
10 mg$943In Stock
25 mg$1,390In Stock
50 mg$1,880In Stock
100 mg$2,560In Stock
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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]
AliasR54718, R 54718, R-54718
Chemical Properties
Molecular Weight373.53
FormulaC22H35N3O2
Cas No.88296-62-2
Storage & Solubility Information
Storage Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility Information
DMSO: 3.74 mg/mL (10 mM)
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

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