同义名 :	-
	CAS号 :	153587-01-0
	货号 :	A900983
	分子式 :	C15H8F6N2O2
	纯度 :	98%+
	分子量 :	362.23
	MDL号 :	MFCD00928190
	存储条件：	Pure form Inert atmosphere, 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

NS-1619 is a selective large conductance Ca2+-activated K+-channel activator. The stimulation of outward currents by NS 1619 at -10 mV was independent of the presence of Ca2+ in the bath or pipette solutions but was antagonized by either charybdotoxin (250 nM) or penitrem A (100 nM) in the bath solution. NS 1619 (3-100 mM) produced a concentration-dependent inhibition of spontaneous activity in rat portal vein characterized by a reduction in the amplitude and duration of the tension waves. NS 1619 activates the large conductance, Ca2+-sensitive channel, BKca and over the same concentration range it inhibits both KV and L-type Ca-channels[3]. NS-1619 induced concentration-dependent activation of BKCa channels with a calculated EC50 of 32 mM. The NS 1619-induced activity was dependent on the presence of free Ca2+ at the intracellular surface, but was not associated with a change in channel voltage sensitivity[4]. When cell membrane voltage was stepped to test potentials (-60 to +60 mV) from a holding potential of -10 mV, NS 1619 increased the outwardly rectifying K+ current in a concentration-dependent manner. NS 1619 reduced electrically stimulated contractile responses of rat vas deferens in a concentration-dependent manner. NS 1619 (10-100 mM) reduced the high K+-induced contractions in a noncompetitive manner[5]. Inhalation of a 12 µM and 100 µM NS1619 solution significantly reduced RV (right ventricular) pressure without affecting systemic arterial pressure. In PASMC's, NS1619 (100 µM) significantly attenuated PASMC proliferation by a pathway independent of AKT and ERK1/2 activation[6].

实验方案
	1mg	5mg	10mg
1 mM 5 mM 10 mM	2.76mL 0.55mL 0.28mL	13.80mL 2.76mL 1.38mL	27.61mL 5.52mL 2.76mL

参考文献

[1]Revermann M, Neofitidou S, et al. Inhalation of the BK(Ca)-opener NS1619 attenuates right ventricular pressure and improves oxygenation in the rat monocrotaline model of pulmonary hypertension. PLoS One. 2014 Jan 31;9(1):e86636. [2]Lee K, Rowe IC, et al. NS 1619 activates BKCa channel activity in rat cortical neurones. Eur J Pharmacol. 1995 Jul 4;280(2):215-9. [3]Edwards G, Niederste-Hollenberg A, Schneider J, Noack T, Weston AH. Ion channel modulation by NS 1619, the putative BKCa channel opener, in vascular smooth muscle. Br J Pharmacol. 1994;113(4):1538-1547 [4]Lee K, Rowe IC, Ashford ML. NS 1619 activates BKCa channel activity in rat cortical neurones. Eur J Pharmacol. 1995;280(2):215-219 [5]Huang Y, Lau CW, Ho IH. NS 1619 activates Ca2+-activated K+ currents in rat vas deferens. Eur J Pharmacol. 1997;325(1):21-27 [6]Revermann M, Neofitidou S, Kirschning T, Schloss M, Brandes RP, Hofstetter C. Inhalation of the BK(Ca)-opener NS1619 attenuates right ventricular pressure and improves oxygenation in the rat monocrotaline model of pulmonary hypertension. PLoS One. 2014;9(1):e86636.