| Cas No.: | 153587-01-0 |
| Chemical Name: | 1,3-Dihydro-1-[2-hydroxy-5-(trifluoromethyl)phenyl]-5-(trifluoromethyl)-2H-benzimidazol-2-one |
| Synonyms: | NS1619,NS 1619 |
| SMILES: | C1=CC2=C(C=C1C(F)(F)F)NC(=O)N2C3=C(C=CC(=C3)C(F)(F)F)O |
| Formula: | C15H8F6N2O2 |
| M.Wt: | 362.23 |
| Purity: | >98% |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | NS-1619 is a selective large conductance Ca2+-activated K+-channel activator.NS 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]. |
| Target: | Ca2+-activated K+-channel activator |
| 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. |
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| LOT NO. | DOWNLOAD |
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| 2018-0101 |
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| 2018-0101 |
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