Biological Activity
Activator of large-conductance Ca2+-activated potassium channels (BKCa, KCa1.1). Exhibits no modulatory effect on a variety of K+ (KV), Na+ and Ca2+ currents at concentrations <10 μM. Alters gating kinetics, but does not affect single channel conductance. Shown to bind BKCa in open and closed conformations; thought to bind the α subunit.
Compound Libraries
NS 11021 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 511.24 |
| Formula | C16H9BrF6N6S |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 956014-19-0 |
| PubChem ID | 24825677 |
| InChI Key | MDKAFDIKYQMOMF-UHFFFAOYSA-N |
| Smiles | BrC1=CC(C2=NN=NN2)=C(NC(NC3=CC(C(F)(F)F)=CC(C(F)(F)F)=C3)=S)C=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 | 51.12 | 100 | |
| ethanol | 51.12 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 511.24. 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 | 1.96 mL | 9.78 mL | 19.56 mL |
| 5 mM | 0.39 mL | 1.96 mL | 3.91 mL |
| 10 mM | 0.2 mL | 0.98 mL | 1.96 mL |
| 50 mM | 0.04 mL | 0.2 mL | 0.39 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Layne et al (2009) BK channel activation by NS11021 decreases excitability and contractility of urinary bladder smooth muscle. Am.J.Physiol.Regul.Integr.Comp.Physiol. 298 R378 PMID: 19923353
Bentzen et al (2007) The small molecule NS11021 is a potent and specific activator of Ca2+-activated big-conductance K+ channels. Mol.Pharmacol. 72 1033 PMID: 17636045
Kun et al (2009) NS11021, a novel opener of large-conductance Ca2+-activated K+ channels, enhances erectile responses in rats. Br.J.Pharmacol. 158 1465 PMID: 19845682
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