Description: Potent and selective Iks channel blocker
Chemical Name:N-[(3R,4S)-3,4-Dihydro-3-hydroxy-2,2-dimethyl-6-(4,4,4-trifluorobutoxy)-2H-1-benzopyran-4-yl]-N-methylmetanesulfonamide
Purity: ≥98% (HPLC)
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
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.
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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Product Datasheets
Certificate of Analysis / Product Datasheet
Safety Datasheet
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References
References are publications that support the products' biological activity.
Gerlachet al (2001) Synthesis and activity of novel and selective I(Ks)-channel blockers. J.Med.Chem. 44 3831 PMID: 11689069
Michaelet 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
Thomaset al (2003) HMR 1556, a potent and selective blocker of slowly activating delayed rectifier potassium current. J.Cardiovasc.Pharmacol. 41 140 PMID: 12500032