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NS1652

Katalog-Nr.GC31133 Copy One-Click Copy Product Info

NS1652 ist ein reversibler AnionenleitfÄhigkeitsinhibitor, der den Chloridkanal blockiert, mit einem IC50 von 1,6 μM in roten BlutkÖrperchen von Mensch und Maus.

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NS1652 Chemische Struktur

Cas No.: 1566-81-0

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Sample solution is provided at 25 µL, 10mM.



Description of NS1652

NS1652 is a reversible anion conductance inhibitor, blocks chloride channel, with an IC50 of 1.6 μM in human and mouse red blood cells.

NS1652 potently inhibits the chloride conductance (IC50, 1.6 μM) in human and mouse red blood cells, but only weakly inhibits VRAC (IC50, 125 μM) in HEK293 cells. NS1652 markedly blocks the NO production with an IC50 of 3.1 μM in BV2 cells. NS1652 also down-regulates iNOS expression at 3 μM, and completely abolishes at 10 μM in BV2 cells[1]. NS1652 (0, 1.0, 3.3, 10, and 20 μM) causes increasing hyperpolarization due to inhibition of the chloride conductance in normal erythrocytes. NS1652 lowers the net KCl loss from deoxygenated sickle cells from about 12 mM cells/h to about 4 mM cells/h. NS1652 (20 μM) completely and reversiblely inhibits the red cell Cl-conductance[2].

NS1652 (50 mg/kg, i.v.) blocks murine erythrocyte Cl- conductance by >90% in mice[2].

[1]. Kjaer K, et al. Chloride channel blockers inhibit iNOS expression and NO production in IFNgamma-stimulated microglial BV2 cells. Brain Res. 2009 Jul 24;1281:15-24. [2]. Bennekou P, et al. Volume control in sickle cells is facilitated by the novel anion conductance inhibitor NS1652. Blood. 2000 Mar 1;95(5):1842-8.

Protocol of NS1652

Animal experiment:

NS1652 is suspended in a carrying vehicle, cremophore (pig-40 hydrogenated castor oil), at a concentration of 5 mg/mL. At time zero, an amount corresponding to 1% of animal weight (about 250 μL of suspension) is injected into mice though the tail veins (NMRI strain, 5-6 weeks). At several time intervals after the injection, the mice are decapitated and the blood collected is collected and centrifuged for 60 seconds. The plasma is removed by aspiration and the packed cells are stored on ice until use. Immediately before measurement, the packed cells are resuspended in 1 volume of ice-cold experimental medium and centrifuged for 30 seconds. A total of 100 μL of packed cells are then immediately transferred to 3 mL medium, and CCCP and valinomycin added. The blood samples are analyzed in random order with respect to the time of decapitation[2].

References:

[1]. Kjaer K, et al. Chloride channel blockers inhibit iNOS expression and NO production in IFNgamma-stimulated microglial BV2 cells. Brain Res. 2009 Jul 24;1281:15-24.
[2]. Bennekou P, et al. Volume control in sickle cells is facilitated by the novel anion conductance inhibitor NS1652. Blood. 2000 Mar 1;95(5):1842-8.

Chemical Properties of NS1652

Cas No. 1566-81-0 SDF
Canonical SMILES O=C(O)C1=CC=CC=C1NC(NC2=CC=CC(C(F)(F)F)=C2)=O
Formula C15H11F3N2O3 M.Wt 324.25
Löslichkeit DMSO: 5 mg/mL (15.42 mM) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of NS1652

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 3.084 mL 15.4202 mL 30.8404 mL
5 mM 616.8 μL 3.084 mL 6.1681 mL
10 mM 308.4 μL 1.542 mL 3.084 mL
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Average Rating: 5 ★★★★★ (Based on Reviews and 31 reference(s) in Google Scholar.)

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