Biological Activity
Selective KV7.2/KV7.3 (KCNQ2/3) channel opener (EC50 = 0.69 μM). Exhibits 20-fold selectivity for KV7.2/KV7.3 over KV7.3/KV7.5, with no measurable activity over a panel of cardiac ion channels. Hyperpolarizes resting membrane potential and inhibits spontaneous action potentials in guinea pig detrusor muscle (DSM) isolated cells. Orally active in animal models of epilepsy.
Compound Libraries
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Technical Data
| M. Wt | 269.63 |
| Formula | C11H6ClF2N3O |
| Storage | Store at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 582323-16-8 |
| PubChem ID | 10149311 |
| InChI Key | IIBSHMFXVWTQSJ-UHFFFAOYSA-N |
| Smiles | ClC1=NC=C(NC(C2=CC(F)=C(F)C=C2)=O)C=N1 |
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 | 26.96 | 100 | |
| ethanol | 6.74 | 25 |
Preparing Stock Solutions
The following data is based on the product molecular weight 269.63. 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 | 3.71 mL | 18.54 mL | 37.09 mL |
| 5 mM | 0.74 mL | 3.71 mL | 7.42 mL |
| 10 mM | 0.37 mL | 1.85 mL | 3.71 mL |
| 50 mM | 0.07 mL | 0.37 mL | 0.74 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Amato et al (2011) N-pyridyl and pyrimidine benzamides as KCNQ2/Q3 potassium channel openers for the treatment of epilepsy. ACS Med.Chem.Lett. 2 481 PMID: 24900334
Provence et al (2015) The novel Kv7.2/Kv7.3 channel opener ICA-069673 reveals subtype-specific functional roles in guinea pig detrusor smooth muscle excitability and contractility. J.Pharmacol.Exp.Ther. 354 290 PMID: 26087697
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