Biological Activity
Potent and selective blocker of KV7 (KCNQ) voltage-gated potassium channels. Blocks KV7.2+7.3 (KCNQ2+3) / M-currents (IC50 = 0.6 - 0.98 μM) and KV7.1 (KCNQ1) homomeric channels (IC50 = 0.75 μM) but is less potent against KV7.1/minK channels (IC50 = 11.1 μM). Augments hippocampal ACh release and is a cognitive enhancer following oral administration in vivo.
Technical Data
| M. Wt | 449.37 |
| Formula | C26H20N2O.2HCl |
| Storage | Desiccate at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 122955-13-9 |
| PubChem ID | 45073462 |
| InChI Key | WOGWMARIFDNZON-UHFFFAOYSA-N |
| Smiles | Cl.Cl.O=C1C2=C(C=CC=C2)C(CC2=CC=NC=C2)(CC2=CC=NC=C2)C2=C1C=CC=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 | |||
| water | 44.94 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 449.37. 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 | 2.23 mL | 11.13 mL | 22.25 mL |
| 5 mM | 0.45 mL | 2.23 mL | 4.45 mL |
| 10 mM | 0.22 mL | 1.11 mL | 2.23 mL |
| 50 mM | 0.04 mL | 0.22 mL | 0.45 mL |
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References
References are publications that support the products' biological activity.
Wang et al (1998) KCNQ2 and KCNQ3 potassium channel subunits: molecular correlates of the M-channel. Science 282 1890 PMID: 9836639
Zaczek et al (1998) Two new potent neurotransmitter release enhancers, 10,10-bis(4-pyridinylmethyl)-9(10H)-anthracenone and 10,10-bis(2-fluoro-4-pyridinylmethyl)-9(10H)-anthracenone: comparison to linopirdine. J.Pharmacol.Exp.Ther. 285 724 PMID: 9580619
Wang et al (2000) Molecular basis for differential sensitivity of KCNQ and IKs channels to the cognitive enhancer XE991. Mol.Pharmacol. 57 1218 PMID: 10825393
Passmore et al (2003) KCNQ/M currents in sensory neurons: significance for pain therapy. J.Neurosci. 23 7227 PMID: 12904483
Keywords: XE 991 dihydrochloride, supplier, KCNQ, channel, blockers, Potassium, KV, Channels, voltage-gated, voltage-dependent, K+, KCNQ2, KCNQ3, KCNQ1, XE991, dihydrochloride, KV7.1, Voltage-Gated, Potassium, Channels, Voltage-Gated, Potassium, Channels, Tocris Bioscience
