NS1652
Based on 1 Customer Validation
NS1652 is a reversible anion conductance inhibitor, blocks chloride channel, with an IC50 of 1.6 μM in human and mouse red blood cells.
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- Pureté: 99.76%
- CAS No.: 1566-81-0
- Formule: C15H11F3N2O3
- Masse moléculaire:324.25
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
IC50: 1.6 μM (chloride channel, human and mouse red blood cell)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
72 μM
Compound: 2a
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In vitro inhibitory activity against human ionotropic glutamate receptor ionotropic kainate 1 (GluR-5) expressed in HEK293 cells.
In vitro inhibitory activity against human ionotropic glutamate receptor ionotropic kainate 1 (GluR-5) expressed in HEK293 cells.
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[PMID: 14667236] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1566-81-0
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Appearance Solid
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Masse moléculaire 324.25
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Formule C15H11F3N2O3
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Color White to off-white
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SMILES
O=C(O)C1=CC=CC=C1NC(NC2=CC=CC(C(F)(F)F)=C2)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvant et solubilité
DMSO : 5 mg/mL (15.42 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocole
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (274 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Instruction de manipulation (2659 KB)
Références
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.0840 mL | 15.4202 mL | 30.8404 mL | 77.1010 mL |
| 5 mM | 0.6168 mL | 3.0840 mL | 6.1681 mL | 15.4202 mL | |
| 10 mM | 0.3084 mL | 1.5420 mL | 3.0840 mL | 7.7101 mL | |
| 15 mM | 0.2056 mL | 1.0280 mL | 2.0560 mL | 5.1401 mL |
NS1652 Related Classifications
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