NS-1619

Modify Date: 2024-01-02 17:49:53

NS-1619 Structure
NS-1619 structure
Common Name NS-1619
CAS Number 153587-01-0 Molecular Weight 362.22700
Density 1.563g/cm3 Boiling Point N/A
Molecular Formula C15H8F6N2O2 Melting Point 234 °C(dec.)
MSDS Chinese USA Flash Point N/A

 Use of NS-1619


NS-1619 is a selective large conductance Ca2+-activated K+-channel activator.IC50 value: Target: Ca2+-activated K+-channel activatorNS 1619 (3-100 microM) 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. This inhibition was slightly potentiated in the presence of either charybdotoxin (250 nM) or penitrem A (1 microM) [1]. NS-1619 induced concentration-dependent activation of BKCa channels with a calculated EC50 of 32 microM. 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 [2]. NS 1619 (50 microM) inhibited the noradrenaline-induced contraction. NS 1619 (10-100 microM) reduced the high K+-induced contractions in a noncompetitive manner [3]. Inhalation of a 12 μM and 100 μM NS1619 solution significantly reduced RV pressure without affecting systemic arterial pressure. Blood gas analyses demonstrated significantly reduced carbon dioxide and improved oxygenation in NS1619-treated animals pointing towards a considerable pulmonary shunt-reducing effect. In PASMC's, NS1619 (100 μM) significantly attenuated PASMC proliferation by a pathway independent of AKT and ERK1/2 activation [4].

 Names

Name ns 1619
Synonym More Synonyms

 NS-1619 Biological Activity

Description NS-1619 is a selective large conductance Ca2+-activated K+-channel activator.IC50 value: Target: Ca2+-activated K+-channel activatorNS 1619 (3-100 microM) 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. This inhibition was slightly potentiated in the presence of either charybdotoxin (250 nM) or penitrem A (1 microM) [1]. NS-1619 induced concentration-dependent activation of BKCa channels with a calculated EC50 of 32 microM. 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 [2]. NS 1619 (50 microM) inhibited the noradrenaline-induced contraction. NS 1619 (10-100 microM) reduced the high K+-induced contractions in a noncompetitive manner [3]. Inhalation of a 12 μM and 100 μM NS1619 solution significantly reduced RV pressure without affecting systemic arterial pressure. Blood gas analyses demonstrated significantly reduced carbon dioxide and improved oxygenation in NS1619-treated animals pointing towards a considerable pulmonary shunt-reducing effect. In PASMC's, NS1619 (100 μM) significantly attenuated PASMC proliferation by a pathway independent of AKT and ERK1/2 activation [4].
Related Catalog
References

[1]. Edwards G, et al. Ion channel modulation by NS 1619, the putative BKCa channel opener, in vascular smooth muscle. Br J Pharmacol. 1994 Dec;113(4):1538-47.

[2]. Lee K, et al. NS 1619 activates BKCa channel activity in rat cortical neurones. Eur J Pharmacol. 1995 Jul 4;280(2):215-9.

[3]. Huang Y, et al. NS 1619 activates Ca2+-activated K+ currents in rat vas deferens. Eur J Pharmacol. 1997 Apr 23;325(1):21-7.

[4]. Revermann M, 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.

 Chemical & Physical Properties

Density 1.563g/cm3
Melting Point 234 °C(dec.)
Molecular Formula C15H8F6N2O2
Molecular Weight 362.22700
Exact Mass 362.04900
PSA 58.02000
LogP 4.06200
Index of Refraction 1.538

 Safety Information

Personal Protective Equipment Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter
RIDADR NONH for all modes of transport
HS Code 2933990090

 Customs

HS Code 2933990090
Summary 2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

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 Synonyms

Lopac-N-170
1-(2-Hydroxy-5-(trifluoromethyl)phenyl)-5-(trifluoromethyl)-1H-benzo[d]imidazol-2(3H)-one
3-[2-hydroxy-5-(trifluoromethyl)phenyl]-6-(trifluoromethyl)-1H-benzimidazol-2-one
1,3-Dihydro-1-[2-hydroxy-5-(trifluoromethyl)phenyl]-5-(trifluoromethyl)-2H-benzimidazol-2-one
NS-1619
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