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XE 991 dihydrochloride

Names

[ CAS No. ]:
122955-13-9

[ Name ]:
XE 991 dihydrochloride

[Synonym ]:
9(10H)-Anthracenone, 10,10-bis(4-pyridinylmethyl)-, hydrochloride (1:2)
10,10-Bis(pyridin-4-ylmethyl)anthracen-9(10H)-one dihydrochloride
NPE-caged-HPTS
10,10-Bis(4-pyridinylmethyl)-9(10H)-anthracenone dihydrochloride

Biological Activity

[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].

[Related Catalog]:

Research Areas >> Neurological Disease
Signaling Pathways >> Membrane Transporter/Ion Channel >> Potassium Channel

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C26H22Cl2N2O

[ Molecular Weight ]:
449.37

[ Exact Mass ]:
448.110931

[ PSA ]:
42.85000

[ LogP ]:
6.39650

[ Storage condition ]:
-20°C

Related Compounds