Biological Activity
High affinity, selective KCa2.2 (SK2) channel blocker (Kd = 3.8 nM). Exhibits >200-fold selectivity for KCa2.2 over KCa2.1, KCa2.3, KCa3.1, IK, Kv and Kir2.1. Increases theta-burst responses and increases LTP in rat hippocampal slices in vitro. Convulsive in vivo.
Technical Data
| M. Wt | 3392.06 |
| Formula | C141H236N46O39S6 |
| Sequence |
AFCNLRXCQLSCRSLGLLGKCIGDKCECVKH (Modifications: X = Dab, Disulfide bridges: 3-21, 8-26, 12-28, His-31 = C-terminal amide) |
| Storage | Store at -20°C |
| CAS Number | 1061556-49-7 |
| Smiles | [H]N[C@@H](C)C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)N[C@H]1CSSC[C@@H]2NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@@H]3CSSC[C@H](NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CSSC[C@H](NC(=O)[C@H]([*])NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(N)=O)NC1=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N3)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(O)=O)NC(=O)CNC(=O)[C@@H](NC2=O)[C@@H](C)CC)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC1=CNC=N1)C(N)=O |
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
| Solubility | Soluble to 1 mg/ml in water |
Preparing Stock Solutions
The following data is based on the product molecular weight 3392.06. 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 | 0.29 mL | 1.47 mL | 2.95 mL |
| 5 mM | 0.06 mL | 0.29 mL | 0.59 mL |
| 10 mM | 0.03 mL | 0.15 mL | 0.29 mL |
| 50 mM | 0.01 mL | 0.03 mL | 0.06 mL |
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References
References are publications that support the products' biological activity.
Shakkottai et al (2001) Design and characterization of a highly selective peptide inhibitor of the small conductance calcium-activated K+ channel, SkCa2. J.Biol.Chem. 276 43145 PMID: 11527975
Kramar et al (2004) A novel mechanism for the facilitation of theta-induced long-term potentiation by brain-derived neurotrophic factor. J.Neurosci. 24 5151 PMID: 15175384
Kasumu et al (2012) Selective positive modulator of calcium-activated potassium channels exerts beneficial effects in a mouse model of spinocerebellar ataxia type 2. Chem.Biol. 19 1340 PMID: 23102227
Keywords: Lei-Dab 7, supplier, Lei-Dab7, selective, potent, small, conductance, calcium, activated, potassium, channels, K+, Ca2+, inhibitors, inhibits, KCa2.2, SK2, blockers, Ca2+-Activated, Potassium, Channels, Ca2+-Activated, Potassium, Channels, Tocris Bioscience
