NS 1619
(Synonyms: 1-(2-羟基-5-(三氟甲基)苯基)-5-(三氟甲基)-1H-苯并[D]咪唑-2(3H)-酮) 目录号 : GC12547
NS 1619是一种选择性的大电导钙激活钾通道激活剂。
Cas No.:153587-01-0
Sample solution is provided at 25 µL, 10mM.
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NS 1619 is a selective large conductance Ca2+-activated K+-channel activator[1]. The Ca²⁺-activated K⁺ channel is a voltage- and Ca²⁺-gated potassium channel that plays a crucial role in regulating cellular excitability and ion homeostasis[2]. NS 1619 is usually used in research on cardiovascular diseases and cancer[3].
In vitro, treatment of A2780 ovarian cancer cells with NS 1619 (5-100μM; 48h) inhibits cell proliferation in a dosage and time-dependent manner, induces cell apoptosis and DNA fragmentation, increases sub-G1 population, augments whole-cell K+ currents, and increases expression of p53, p21, and Bax proteins[4]. Treatment of rat ventricular myocytes with NS 1619 (10μM; 2min) inhibits L-type Ca²⁺ channels in a dose-dependent manner, and shifts the activation curve to more positive potentials but does not significantly affect the inactivation curve[5].
In vivo, NS 1619 (1mg/kg; i.p.) significantly reduced leukocyte rolling and adhesion, prevented increases in intestinal TNFα levels, and preserved mucosal barrier function in wild-type C57BL/6J mice with intestinal ischemia/reperfusion injury[6]. NS 1619 (1mg/kg; i.p.; 24 hours before ischemia/reperfusion) significantly reduced infarct size and improved postischemic ventricular function in adult male ICR mice[7].
References:
[1] 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.
[2] Latorre R, Brauchi S. Large conductance Ca2+-activated K+ (BK) channel: activation by Ca2+ and voltage. Biol Res. 2006;39(3):385-401.
[3] 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.
[4] Han X, Xi L, Wang H, et al. The potassium ion channel opener NS1619 inhibits proliferation and induces apoptosis in A2780 ovarian cancer cells. Biochem Biophys Res Commun. 2008;375(2):205-209.
[5] Park WS, Kang SH, Son YK, et al. The mitochondrial Ca2+-activated K+ channel activator, NS 1619 inhibits L-type Ca2+ channels in rat ventricular myocytes. Biochem Biophys Res Commun. 2007;362(1):31-36.
[6] Dai H, Wang M, Patel PN, et al. Preconditioning with the BKCa channel activator NS-1619 prevents ischemia-reperfusion-induced inflammation and mucosal barrier dysfunction: roles for ROS and heme oxygenase-1. Am J Physiol Heart Circ Physiol. 2017;313(5):H988-H999.
[7] Wang X, Yin C, Xi L, Kukreja RC. Opening of Ca2+-activated K+ channels triggers early and delayed preconditioning against I/R injury independent of NOS in mice. Am J Physiol Heart Circ Physiol. 2004;287(5):H2070-H2077.
NS 1619是一种选择性的大电导钙激活钾通道激活剂[1]。钙激活钾通道是一种电压和钙离子门控的钾通道，在调节细胞兴奋性和离子稳态中发挥关键作用[2]。NS 1619常用于心血管疾病和癌症的研究[3]。
在体外，NS 1619 (5-100μM； 48小时) 处理A2780卵巢癌细胞以剂量和时间依赖的方式抑制细胞增殖，诱导细胞凋亡、DNA 片段化，增加sub-G1期细胞比例，增强全细胞K⁺电流，并提高 p53、p21和Bax蛋白的表达[4]。NS 1619（10μM；2分钟）处理大鼠心室肌细胞可剂量依赖性地抑制L型Ca²⁺通道，使激活曲线向更正的电位方向移动，但对失活曲线无显著影响[5]。
在体内，NS 1619（1mg/kg；腹腔注射）可在野生型C57BL/6J小鼠的肠道缺血/再灌注损伤模型中显著减少白细胞滚动和黏附，抑制肠道 TNFα水平升高，并维持黏膜屏障功能[6]。NS 1619（1mg/kg；腹腔注射；缺血/再灌注前24小时给药）可显著减少成年雄性ICR小鼠的心肌梗死面积并改善缺血后的心室功能[7]。
| Cell experiment [1]: | |
Cell lines | Human ovarian cancer A2780 cells |
Preparation Method | The human ovarian cancer A2780 cells were cultured in RPMI 1640 supplemented with 10% fetal bovine serum at 37℃ under 5% CO2 in a humidified incubator. Cells were seeded in 96-well plates (6000cells/well) and the final volume of cell culture medium in each well was 0.1ml. The following day, cells were treated with various concentrations (5, 10, 30, 50, and 100μM) of NS 1619 for 48h. The effect of NS 1619 on cancer cell proliferation was evaluated by using the MTT colorimetric assay. The cultured cells were mounted on the stage of an inverted microscope and whole-cell K+ currents were recorded using glass pipettes pulled from a vertical puller and an EPC-9 patch-clamp amplifier. Fragmented DNA was analysed by agarose gel electrophoresis. Flow cytometry was used for cell apoptosis analysis. Proteins were extracted for west blotting analysis. |
Reaction Conditions | 5-100μM; 48h |
Applications | Treatment of A2780 ovarian cancer cells with NS 1619 inhibits cell proliferation in a dosage and time-dependent manner, induces cell apoptosis and DNA fragmentation, increases sub-G1 population, augments whole-cell K+ currents, and increases expression of p53, p21, and Bax proteins. |
| Animal experiment [2]: | |
Animal models | Adult male outbred ICR mice |
Preparation Method | Adult male outbred ICR mice were randomly assigned to two groups: Control group: mice received an intraperitoneal injection of 0.15ml of 1% DMSO 24h before heart isolation and ischemia/reperfusion (I/R); Expriment group: mice were pretreated with NS 1619 (1mg/kg; i.p.) 24h before I/R. No-flow global ischemia was attained by completely stopping the perfusate inflow. Reperfusion was achieved by reopening the buffer-perfusion line. Ventricular contractile force was continuously measured with a force-displacement transducer attached to the apex of the heart and was recorded and analyzed with a computerized data acquisition and analysis system. The heart temperature was precisely maintained at 37°C throughout the experiment. Coronary flow rate was measured by timed collection of the outflow coronary perfusate. At the end of reperfusion, the heart was immediately removed from the perfusion apparatus, weighed, and stored overnight at -20°C for myocardial infarct size analysis. |
Dosage form | 1mg/kg; i.p.; 24 hours before ischemia/reperfusion |
Applications | NS 1619 significantly reduced infarct size and improved postischemic ventricular function in adult male ICR mice. |
References: | |
| Cas No. | 153587-01-0 | SDF | |
| 别名 | 1-(2-羟基-5-(三氟甲基)苯基)-5-(三氟甲基)-1H-苯并[D]咪唑-2(3H)-酮 | ||
| 化学名 | 1-(2-hydroxy-5-(trifluoromethyl)phenyl)-5-(trifluoromethyl)-1H-benzo[d]imidazol-2(3H)-one | ||
| Canonical SMILES | FC(F)(C1=CC=C(C(NC2=O)=C1)N2C(C=C(C(F)(F)F)C=C3)=C3O)F | ||
| 分子式 | C15H8F6N2O2 | 分子量 | 362.23 |
| 溶解度 | ≥ 72.4mg/mL in DMSO | 储存条件 | Store at -20°C |
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.7607 mL | 13.8034 mL | 27.6068 mL |
| 5 mM | 552.1 μL | 2.7607 mL | 5.5214 mL |
| 10 mM | 276.1 μL | 1.3803 mL | 2.7607 mL |
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