同义名 :	XE 991 (hydrochloride); XE991 dihydrochloride; LS190926 dihydrochloride
	CAS号 :	122955-13-9
	货号 :	A268758
	分子式 :	C26H22Cl2N2O
	纯度 :	99%+
	分子量 :	449.37
	MDL号 :	MFCD09055426
	存储条件：	Pure form Sealed in dry,2-8°C In solvent -20°C:3-6个月-80°C:12个月
	溶解度 :	-
	动物实验配方：

生物活性

描述

XE 991 2HCl (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[3]. XE991 and DMP 543 may prove to be superior to linopirdine as Alzheimer's disease therapeutics. Although linopirdine possesses an EC50 of 4.2 microM for enhancement of [3H]ACh release from rat brain slices, XE991 and DMP 543 have EC50S of 490 and 700 nM, respectively. Although 5 mg/kg (p.o.) linopirdine does not lead to statistically significant increases in hippocampal extracellular acetylcholine levels, 5 mg/kg (p.o.) XE991 leads to increases (maximal effect > 90% over baseline) which are sustained for 60 min[4]. XE991 at 30 μM reduced the anti-contractile response of PVAT, but had no effects on vasocontraction induced by phenylephrine (PE) in the absence of PVAT (perivascular adipose tissue). 30 μM XE991 did not affect BKCa currents in VSMCs[5].

实验方案
	1mg	5mg	10mg
1 mM 5 mM 10 mM	2.23mL 0.45mL 0.22mL	11.13mL 2.23mL 1.11mL	22.25mL 4.45mL 2.23mL

参考文献

[1]Greene DL, Kang S, Hoshi N. XE991 and Linopirdine are state-dependent inhibitors for Kv7/KCNQ channels that favor activated single subunits. J Pharmacol Exp Ther. 2017 May 8. pii: jpet.117.241679. [2]Greene DL, Kang S, Hoshi N. XE991 and Linopirdine are state-dependent inhibitors for Kv7/KCNQ channels that favor activated single subunits. J Pharmacol Exp Ther. 2017 May 8. pii: jpet.117.241679. [3]Wang HS, Pan Z, Shi W, Brown BS, Wymore RS, Cohen IS, Dixon JE, McKinnon D. KCNQ2 and KCNQ3 potassium channel subunits: molecular correlates of the M-channel. Science. 1998 Dec 4;282(5395):1890-3 [4]Zaczek R, Chorvat RJ, Saye JA, Pierdomenico ME, Maciag CM, Logue AR, Fisher BN, Rominger DH, Earl RA. 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 [5]Tsvetkov D, Tano JY, Kassmann M, Wang N, Schubert R, Gollasch M. The Role of DPO-1 and XE991-Sensitive Potassium Channels in Perivascular Adipose Tissue-Mediated Regulation of Vascular Tone. Front Physiol. 2016 Aug 4;7:335