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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 Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $161 | In Stock | In Stock | |
| 5 mg | $398 | In Stock | In Stock | |
| 10 mg | $566 | In Stock | In Stock | |
| 25 mg | $833 | In Stock | In Stock |
| 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 | R-54718, R54718, R 54718 |
| Molecular Weight | 373.53 |
| Formula | C22H35N3O2 |
| Cas No. | 88296-62-2 |
| Smiles | C(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 | Powder: -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
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Dissolve 2 mg of the compound in 100 μL DMSO
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.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
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 ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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