107254-86-4|NPPB|CsnPharm

CAS No.: 107254-86-4

NPPB/5-硝基-2-(3-苯丙胺)苯甲酸 Catalog No. CSN21767

Synonyms: HOE 144;Hoechst 144

NPPB can act as a blocker of the chloride channel with IC50 of 100 nM-100 µM and inhibitor of cyclooxygenase (IC50 = 8 µM).

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技术信息

生物活性

描述NPPB is a blocker of the outwardly rectifying chloride channel (ORCC). Dose-dependent inhibition of chloride currents is observed with a 50% inhibitory concentration (IC50) of 125 μM NPPB. NPPB itself also shows cytotoxicity against glioma cells with a GI50 of approximately 500 μM. TMZ(Temozolomide)-NPPB blocked chloride currents in U373MG, a severely invasive human glioma cell line, and suppressed migration and invasion of U373MG cells^[1]. NPPB treatment inhibited proliferation, migration, cell cycle progression and synthesis of the ECM(extracellular matrix), while promoting apoptosis in HConFs(human conjunctival fibroblasts), by inhibiting the PI3K̸AKT(phosphoinositide 3-kinase/protein kinase B) signaling pathway^[2]. NPPB triggered Ca(2+) efflux from mature zone of tea root and significantly increased relative CaM in tea roots. Besides, pretreatment with the Ca(2+) chelator (EGTA) and CaM antagonists (CPZ and TFP) suppressed NPPB-elevated cytosolic Ca(2+) fluorescence intensity and CaM concentration in tea roots, respectively^[3]. NPPB could significantly prevent the formation of peritoneal adhesion in rats and inhibit the proliferation of AFB in a concentration-dependent manner. NPPB also reduced the migration of AFB (adhesion fibroblasts) cells with an IC50 of 53.09 μM. Moreover, 100 μM NPPB almost completely eliminated the capacity of regulatory volume decrease (RVD) in these cells^[4].
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT01355380	-	-	Completed	-	Poland ... more >> Many Locations, Poland Collapse <<
NCT00586027	-	-	Completed	-	Germany ... more >> Klinikum der Stadt Ludwigshafen, Department of Anesthesiology and Intensive Care Medicine Ludwigshafen, Germany, 67063 Collapse <<
NCT02792452	-	-	Recruiting	July 2018	United Kingdom ... more >> Northwick Park Hospital Recruiting Harrow, MIddx, United Kingdom, HA1 3UJ Contact: Anastasia Vamvakidou 0208 869 2547 anastasia.vamvakidou@nhs.net Contact: Ann Banfield 0208 869 2547 annbanfield@nhs.net Collapse <<

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参考文献

[1] Park M, Song C, Yoon H, Choi KH. Double Blockade of Glioma Cell Proliferation and Migration by Temozolomide Conjugated with NPPB, a Chloride Channel Blocker. ACS Chem Neurosci. 2016;7(3):275‐285
[2] Sun L, Dong Y, Zhao J, et al. NPPB modulates apoptosis, proliferation, migration and extracellular matrix synthesis of conjunctival fibroblasts by inhibiting PI3K/AKT signaling. Int J Mol Med. 2018;41(3):1331‐1338
[3] Zhang XC, Gao HJ, Yang TY, et al. Anion Channel Inhibitor NPPB-Inhibited Fluoride Accumulation in Tea Plant (Camellia sinensis) Is Related to the Regulation of Ca²⁺, CaM and Depolarization of Plasma Membrane Potential. Int J Mol Sci. 2016;17(1):57. Published 2016 Jan 5
[4] Zhong J, Qin Z, Yu H, et al. NPPB prevents postoperative peritoneal adhesion formation by blocking volume-activated Cl- current. Naunyn Schmiedebergs Arch Pharmacol. 2020;393(3):501‐510

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.3299 mL
- 16.6495 mL
- 33.2990 mL
- 5 mM
- 0.6660 mL
- 3.3299 mL
- 6.6598 mL
- 10 mM
- 0.3330 mL
- 1.6650 mL
- 3.3299 mL

技术信息

CAS号

107254-86-4

储存条件

粉末: Keep in dark place,Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C16H16N2O4

运输

蓝冰

分子量

300.31

别名

HOE 144;Hoechst 144

溶解度

DMSO	230.0 mg/mL (765.9 mM)
Water	insoluble

动物实验配方

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NPPB/5-硝基-2-(3-苯丙胺)苯甲酸 Catalog No. CSN21767

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