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1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemENPPBCat. No.: HY-101012CAS No.: 107254-86-4Synonyms: 5-Nitro-2-(3-phenylpropylamino)benzoic acid; Hoechst 144;HOE 144分式: CHNO分量: 300.31作靶点: Chloride Channel作通路: Membrane Transporter/Ion Channel储存式: Powder -20C 3 years4C 2 yearsI

2、n solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 150 mg/mL (499.48 mM; Need ultrasonic and warming)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 3.3299 mL 16.6495 mL 33.2989 mL5 mM 0.6660 mL 3.3299 mL 6.6598 mL10 mM 0.3330 mL 1.6649 mL 3.3299 mL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,并请注意储备液的保存式和期限。体内实

3、验 请根据您的实验动物和给药式选择适当的溶解案,配制前请先配制澄清的储备液,再依次添加助溶剂(为保证实验结果的可靠性,体内实验的作液,建议您现现配,当天使;澄清的储备液可以根据储存条件,适当保存;以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占):1. 请依序添加每种溶剂: 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (8.32 mM); Clear solution1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性

4、NPPB是外向整流氯化物通道 (ORCC) 的阻断剂。IC50 & Target ORCC 1体外研究 0.1 mM NPPB in the bath solution reduces channel open probability from 0.890.06 to 0.110.04 (n=5, P 1.Dose-dependent inhibition of chloride currents is observed with a 50% inhibitory concentration (IC50) of 125M NPPB. NPPB itself also shows cytotox

5、icity against glioma cells with a GI50 of approximately 500 M 2.PROTOCOLCell Assay 2 Cells are seeded in the 96-well microtiter plate at a density of 5103 cells per well and incubated at 37C for24 h in a humidified 5% CO2 atmosphere. After removing the culture medium, fresh media containing variousc

6、oncentrations of NPPB is added, and incubated for 24 h. Next, 100 L of Thiazolyl blue tetrazolium bromideat 0.5 mg/mL is added to each well and incubated at 37C for 1 h. Cells are then dissolved in 100 L ofDMSO, and the absorbance is measured at 570 nm with a Microplate Reader. Concentration-respons

7、ecurves of NPPB are fitted to a Hill equation to obtain GI50 and GI80 (50% and 80% growth inhibitionconcentrations, respectively) values 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Li J, et al. Enhancement of an outwardly rectifying c

8、hloride channel in hippocampal pyramidal neurons after cerebral ischemia. BrainRes. 2016 Aug 1;1644:107-17.2. Park M, et al. Double Blockade of Glioma Cell Proliferation and Migration by Temozolomide Conjugated withNPPB, a Chloride ChannelBlocker. ACS Chem Neurosci. 2016 Mar 16;7(3):275-85.McePdfHeightCaution: Product has not been fully validated for medical applications

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