Biological Activity
Potent and selective Iks channel blocker (IC50 values are 10.5 and 34 nM in canine and guinea pig ventricular myocytes respectively). Selectively inhibits IKs currents over IKr, IKI, Ito and L-type Ca2+ channel currents. Also has little or no effect on Kv11.1 Kv1.5, Kv1.3, Kir2.1 and HCN2 channel currents. Potentiates E-4031-induced arrhythmias in vivo.
Technical Data
| M. Wt | 411.44 |
| Formula | C17H24F3NO5S |
| Storage | Store at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 223749-46-0 |
| PubChem ID | 9887834 |
| InChI Key | SRZRLJWUQFIZRH-LSDHHAIUSA-N |
| Smiles | CC2(C)[C@H](O)[C@@H](N(S(C)(=O)=O)C)C1=CC(OCCCC(F)(F)F)=CC=C1O2 |
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 | 41.14 | 100 | |
| ethanol | 8.23 | 20 |
Preparing Stock Solutions
The following data is based on the product molecular weight 411.44. 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 | 2.43 mL | 12.15 mL | 24.3 mL |
| 5 mM | 0.49 mL | 2.43 mL | 4.86 mL |
| 10 mM | 0.24 mL | 1.22 mL | 2.43 mL |
| 50 mM | 0.05 mL | 0.24 mL | 0.49 mL |
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References
References are publications that support the products' biological activity.
Gerlach et al (2001) Synthesis and activity of novel and selective I(Ks)-channel blockers. J.Med.Chem. 44 3831 PMID: 11689069
Michael et al (2007) Potentiation of E-4031-induced torsade de pointes by HMR1556 or ATX-II is not predicted by action potential short-term variability or triangulation. Br.J.Pharmacol 152 1215 PMID: 17965747
Thomas et al (2003) HMR 1556, a potent and selective blocker of slowly activating delayed rectifier potassium current. J.Cardiovasc.Pharmacol. 41 140 PMID: 12500032
Keywords: HMR 1556, supplier, HMR1556, potent, selective, IKs, channels, blockers, blocks, cardiac, Kv7.1, potassium, K+, slow, delayed, rectifier, current, KCNQ1, voltage-gated, voltage-dependent, Voltage-Gated, Potassium, Channels, Voltage-Gated, Potassium, Channels, Tocris Bioscience
