Biological Activity
Potent IKs blocker (IC50 = 64 nM). Displays no effects on other cardiac channels; IC50 values are 3.3, >10, 11.1 and 12.6 μM for INa, ICa, Ito and IKr currents respectively. Prolongs QT and causes unprovoked torsades de pointes (TdP).
Licensing Information
Sold with the permission of Janssen Pharmaceutica NV
Technical Data
| M. Wt | 440.98 |
| Formula | C21H29ClN2O4S |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 878489-28-2 |
| PubChem ID | 73016713 |
| InChI Key | OSGIRCJRKSAODN-UHFFFAOYSA-N |
| Smiles | O=C(C(C)(C)OC4=CC=C(Cl)C=C4)NC2C1CC(CC2C3)CC3(NS(=O)(C)=O)C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 11.02 | 25 |
Preparing Stock Solutions
The following data is based on the product molecular weight 440.98. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.27 mL | 11.34 mL | 22.68 mL |
| 5 mM | 0.45 mL | 2.27 mL | 4.54 mL |
| 10 mM | 0.23 mL | 1.13 mL | 2.27 mL |
| 50 mM | 0.05 mL | 0.23 mL | 0.45 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Towart et al (2009) Blockade of the IKs potassium channel: an overlooked cardiovascular liability in drug safety screening? J.Pharm.Toxicol.Meth 60 1 PMID:
Keywords: JNJ 303, supplier, potent, Iks, blockers, JNJ303, potassium, K+, channels, selective, slow, delayed, rectifier, current, KCNQ1, Kv7.1, voltage-gated, voltage-dependent, Voltage-Gated, Potassium, Channels, Voltage-Gated, Potassium, Channels, Tocris Bioscience
