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XE 991 dihydrochloride

  Cat. No.:  DC21827   Featured
Chemical Structure
122955-13-9
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More than 5000 active chemicals with high quality for research!
Field of application
A potent, selective and orally active blocker of voltage-gated potassium channels Kv7 (KCNQ) that blocks KCNQ1, KCNQ2 and KCNQ2+KCNQ3 with Kd of 0.78, 0.7 and 0.6 uM, respectively.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 122955-13-9
Chemical Name: 10,10-bis(4-Pyridinylmethyl)-9(10H)-anthracenone dihydrochloride
Synonyms: XE-991;XE991
SMILES: Cl.Cl.N1=CC=C(C=C1)CC2(CC3=CC=NC=C3)C4C(=CC=CC=4)C(=O)C5C2=CC=CC=5
Formula: C26H20N2O.2HCl
M.Wt: 449.37
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication: [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.
Description: 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)[1]
In Vitro: 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].
References: [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
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