| Bioactivity | XE 991 dihydrochloride, a Kv7 (KCNQ) channels blocker, potently inhibits Kv7.1 (KCNQ1), Kv7.2 (KCNQ2), Kv7.2 + Kv7.3 (KCNQ3) channel, and M-current with IC50s of 0.75 µM, 0.71 µM, 0.6 μM, and 0.98 µM, respectively[1]. |
| Target | IC50: 0.75 µM ( Kv7.1 channel), 0.71 µM (Kv7.2 channel), 0.6 µM (Kv7.2 + Kv7.3 channel), 0.98 μM (M-current) |
| Invitro | XE 991 dihydrochloride possesses an EC50 of 490 nM for enhancement of [3H]ACh release from rat brain slices, and shows good in vivo potency and duration of action[2]. |
| Name | XE 991 dihydrochloride |
| CAS | 122955-13-9 |
| Formula | C26H22Cl2N2O |
| Molar Mass | 449.37 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| Reference | [1]. Wang HS, et al. KCNQ2 and KCNQ3 potassium channel subunits: molecular correlates of the M-channel. Science. 1998 Dec 4;282(5395):1890-3. [2]. Zaczek R, et al. 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. 1998 May;285(2):724-30. |