Name: NS-1619
Brand: Alomone Labs
SKU: N-105
Availability: InStock

Cat #: N-105

Lyophilized Powder yes

Bioassay Tested

Source Synthetic

MW: 362.2

Purity: >95%

Effective concentration 100 nM - 100 μM.

Structure

Chemical name 1,3-Dihydro-1-[2-hydroxy-5-(trifluoromethyl)phenyl]-5-(trifluoromethyl)-2H-benzimidazol-2-one.

Molecular formula C₁₅H₈F₆N₂O₂.

CAS No.: 153587-01-0

Activity NS-1619 is a potent and selective K_Ca1.1 (BK, slo, Large conductance Ca²⁺-activated K⁺) channel modulator (enhancer)¹. NS-1619 was effective in eliciting and enhancing K_Ca1.1 channels in smooth muscle as well as in neurons with maximal effects at concentrations around 30 μM^1,2. NS-1619 was used in vivo by intracarotid infusion and significantly enhanced blood tumor barrier permeability in the brain tumor area but not in normal brain tissue³.

References-Activity

Edwards, G. et al. (1994) Br. J. Pharmacol. 113, 1538.
Sellers, A.G. and Ashford, L.M.J. (1994) Br. J. Pharmacol. 113, 659.
Ningaraj, N.S. et al. (2002) J. Pharmacol. Exp. Ther. 301, 838.

Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.

Solubility DMSO. Centrifuge all product preparations before use (10000 x g 5 min).

Storage of solutions Up to four weeks at 4°C or three months at -20°C.

Our bioassay

Alomone Labs NS-1619 enhances K_Ca1.1 currents in Xenopus oocytes.
A. Families of K_Ca1.1 channel current responses to increasing voltage step stimulation (from -50 mV to + 50 mV), before (left) and during (right) application of 100 μM NS-1619 (#N-105). Currents were elicited by 100 ms voltage step from -100 mV applied every 10 sec. B. Time course of current amplitude at 0 mV before, during application of 100 μM NS-1619 (green) and upon wash, demonstrating the current amplitude enhancement. C. Voltage dependence of K_Ca1.1 channel activity enhancement.

References - Scientific background

Andersson K.E. et al. (2004) Physiol. Rev. 84, 935.
Heppner, T.J. et al. (1997) Am. J. Physiol. 273, C110.
Salkoff, L. et al. (2006) Nat. Rev. Neurosci. 7, 921.
Olesen S.P. et al. (1994) Eur. J. Pharmacol. 251, 53.
Holland M. et al. (1996) Br. J. Pharmacol. 117, 119.
Macmillan S. et al. (1995) Br. J. Pharmacol. 116, 1656.
Yamamura H. et al. (2001) Br. J. Pharmacol. 132, 828.
Han X. et al. (2008) Biochem. Biophys. Res. Commun. 375, 205.
Wrzosek, A. (2014) Cell Calcium 56, 14.

Scientific background

The large conductance voltage- and Ca²⁺-activated K⁺ (BK) channels, also known as BK_Ca, K_Ca1.1, Slo, or MaxiK, play an important role in modulating nerve and muscle cell contractility and excitability^1-3. BK channels are activated by both depolarizing voltages and by an increase in intracellular free Ca²⁺, thus coupling the membrane potential to intracellular signaling.

NS-1619 is a potent and selective K_Ca1.1 channel modulator (enhancer)⁴. It has the potential to modulate cell excitability in neurons and smooth muscle^5-7. The effect of relaxation of NS-1619 on the BK channel in smooth muscle cells has an EC₅₀ of 10–30 µM. It is also dose-dependent, resulting in a shift of the activation curve by up to -50 mV towards negative membrane potentials, but fully reversible⁸.

NS-1619 also modulates intracellular Ca²⁺ by inhibiting SERCA pumps⁹.

Target K_Ca1.1 K⁺ channels, SERCA pumps

Lyophilized Powder

Last update: 08/06/2021

NS-1619 (#N-105) is a highly pure, synthetic, and biologically active compound.

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NS-1619

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Scientific Background

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