NS-1619

Names

[ Name ]:
NS-1619

[Synonym ]:
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

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]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> Potassium Channel

Research Areas >> Cardiovascular Disease

[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.

[Related Small Molecules]

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

MSDS

Click to get detail MSDS

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%

Articles

Potassium channel openers prevent palmitate-induced insulin resistance in C2C12 myotubes.

Arch. Biochem. Biophys. 541 , 47-52, (2014)

Insulin resistance (IR) of muscle cells is an early symptom of type 2 diabetes. It often results from excessive lipid accumulation in muscle fibers which under in vitro experimental conditions may be ...

Potassium ion channels and allergic asthma.

Adv. Exp. Med. Biol. 838 , 35-45, (2015)

High-conductive calcium-sensitive potassium channels (BK+Ca) and ATP-sensitive potassium (K+ATP) channels play a significant role in the airway smooth muscle cell and goblet cell function, and cytokin...

High glucose alters apoptosis and proliferation in HEK293 cells by inhibition of cloned BK Ca channel.

J. Cell Physiol. 226(6) , 1660-75, (2011)

It has been reported that diabetic vascular dysfunction is associated with impaired function of large conductance Ca(2+) -activated K(+) (BK(Ca) ) channels. However, it is unclear whether impaired BK(...

Related Compounds

The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.