Biological Activity
Selective KCa2 (SK) channel negative modulator; inhibits SK channel currents (Kd values are 0.42, 0.6 and 0.73 μM for SK1, SK2 and SK3 respectively at 0.5 μM Ca2+). Exhibits selectivity for SK channels over KCa1.1 (BK), KCa3.1 (IK), Kv, Nav and Cav channels. Inhibits afterhyperpolarization in hippocampal slices.
Compound Libraries
NS 8593 hydrochloride is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 299.8 |
| Formula | C17H17N3.HCl |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 875755-24-1 |
| PubChem ID | 71311765 |
| InChI Key | VWEKCDTXUUPBNA-PFEQFJNWSA-N |
| Smiles | C12=CC=CC=C1N=C(N[C@H]3C(C=CC=C4)=C4CCC3)N2.Cl |
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 | 29.98 | 100 | |
| ethanol | 6 | 20 |
Preparing Stock Solutions
The following data is based on the product molecular weight 299.8. 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 | 3.34 mL | 16.68 mL | 33.36 mL |
| 5 mM | 0.67 mL | 3.34 mL | 6.67 mL |
| 10 mM | 0.33 mL | 1.67 mL | 3.34 mL |
| 50 mM | 0.07 mL | 0.33 mL | 0.67 mL |
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References
References are publications that support the products' biological activity.
Strøbaek et al (2006) Inhibitory gating modulation of small conductance Ca2+-activated K+ channels by the synthetic compound (R)-N-(benzimidazol-2-yl)-1,2,3,4-tetrahydro-1-naphtylamine (NS8593) reduces afterhyperpolarizing current in hip Mol.Pharmacol. 70 1771 PMID: 16926279
Sørensen (2008) Synthesis and structure-activity relationship studies of 2-(N-substituted)-aminobenzimidazoles as potent negative gating modulators of small conductance Ca2+-activated K+ channels. J.Med.Chem. 51 7625 PMID: 18998663
Jenkins et al (2011) Negative gating modulation by (R)-N-(benzimidazol-2-yl)-1,2,3,4-tetrahydro-1-naphthylamine (NS8593) depends on residues in the inner pore vestibule: pharmacological evidence of deep-pore gating of KCa2 channels. Mol.Pharmacol. 79 899 PMID: 21363929
Keywords: NS 8593 hydrochloride, supplier, NS8593, hydrochloride, selective, Kca2, SK, small, channels, conductance, calcium, ca2+, activated, potassium, K+, modulators, inhibits, inhibitors, Ca2+-Activated, Potassium, Channels, Ca2+-Activated, Potassium, Channels, Tocris Bioscience
