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Transcainide

Catalog No. T26287 CAS 88296-62-2

Synonyms: R54718, R 54718, 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.

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Transcainide, CAS 88296-62-2

Pack Size	Availability	Price/USD
1 mg	In stock	$ 268.00
5 mg	In stock	$ 663.00
10 mg	In stock	$ 943.00
25 mg	In stock	$ 1,390.00
50 mg	In stock	$ 1,880.00
100 mg	In stock	$ 2,560.00

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Purity: 100%

Biological Description

Chemical Properties

Storage & Solubility Information

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]

Synonyms	R54718, R 54718, R-54718
Molecular Weight	373.53
Formula	C22H35N3O2
CAS No.	88296-62-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 3.74 mg/mL (10 mM), Sonication is recommended.

References and Literature

1. Hill RJ, et al. Transcainide: biochemical evidence for state-dependent interaction with the class I antiarrhythmic drug receptor. Eur J Pharmacol. 1991 Oct 2;203(1):51-8. 2. Bennett PB, et al. Sodium channel block by a potent, new antiarrhythmic agent, transcainide, in guinea pig ventricular myocytes. J Cardiovasc Pharmacol. 1987 Jun;9(6):661-7. 3. Carmeliet E, et al. Electrophysiologic, antiarrhythmic and hemodynamic effects of transcainide. Arch Int Pharmacodyn Ther. 1987 Jun;287(2):272-90. 4. Zamponi GW, et al. Transcainide causes two modes of open-channel block with different voltage sensitivities in batrachotoxin-activated sodium channels. Biophys J. 1994 Sep;67(3):1028-39.

Related compound libraries

This product is contained In the following compound libraries：

Membrane Protein-targeted Compound Library Bioactive Compound Library Bioactive Compounds Library Max

Related Products

Related compounds with same targets

Sodium Channel inhibitor 4 Fosphenytoin disodium β-Pompilidotoxin Acetate Pterinotoxin-1 AZD 7009 PF 05089771 Ancistrotecine B Wilfordine

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Keywords

Transcainide 88296-62-2 Membrane transporter/Ion channel Sodium Channel R54718 R 54718 R-54718 inhibitor inhibit

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