NS1652
目录号 : GC31133
NS1652是一种可逆的阴离子电导(anionconductance)抑制剂，在人和小鼠的红细胞中，可以抑制氯离子通道(chloridechannel)，IC50值为1.6μM。
Cas No.:1566-81-0
Sample solution is provided at 25 µL, 10mM.
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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.
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. | |
| Cas No. | 1566-81-0 | SDF | |
| Canonical SMILES | O=C(O)C1=CC=CC=C1NC(NC2=CC=CC(C(F)(F)F)=C2)=O | ||
| 分子式 | C15H11F3N2O3 | 分子量 | 324.25 |
| 溶解度 | DMSO: 5 mg/mL (15.42 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.084 mL | 15.4202 mL | 30.8404 mL |
| 5 mM | 0.6168 mL | 3.084 mL | 6.1681 mL |
| 10 mM | 0.3084 mL | 1.542 mL | 3.084 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet