Biological Activity
Potent KV1.3 channel blocker (EC50 = 3 nM). Preferentially binds the C-type inactivated state of the channel, similar to the activity of CP 339818 (Cat. No. 1399). Displays 17- to 70-fold selectivity over closely-related KV1 channels (KV1, KV2, KV4 and KV7); exhibits activity at KV1.5 (IC50 = 7.7 nM). Suppresses proliferation of human and rat myelin-specific effector memory T cells (EC50 values are 25 and 60 nM respectively).
Technical Data
| M. Wt | 334.37 |
| Formula | C21H18O4 |
| Storage | Store at -20°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 724709-68-6 |
| PubChem ID | 6603977 |
| InChI Key | JJAWGNIQEOFURP-UHFFFAOYSA-N |
| Smiles | O=C2OC1=CC3=C(C=CO3)C(OCCCCC4=CC=CC=C4)=C1C=C2 |
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 | 16.72 | 50 | |
| ethanol | 3.34 | 10 |
Preparing Stock Solutions
The following data is based on the product molecular weight 334.37. 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 | 2.99 mL | 14.95 mL | 29.91 mL |
| 5 mM | 0.6 mL | 2.99 mL | 5.98 mL |
| 10 mM | 0.3 mL | 1.5 mL | 2.99 mL |
| 50 mM | 0.06 mL | 0.3 mL | 0.6 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Vennekamp et al (2004) Kv1.3-blocking 5-phenylalkoxypsoralens: a new class of immunomodulators. Mol.Pharmacol. 65 1364 PMID: 15155830
Schmitz et al (2005) Design of PAP-1, a selective small molecule Kv1.3 blocker, for the suppression of effector memory T cells in autoimmune diseases. Mol.Pharmacol. 68 1254 PMID: 16099841
Li et al (2006) Voltage-gated potassium channel Kv1.3 regulates GLUT4 trafficking to the plasma membrane via a Ca2+-dependent mechanism. Am.J.Physiol.Cell Physiol. 290 C345 PMID: 16403947
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