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NPPB

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Chemical Structure| 107254-86-4 同义名 : HOE 144;Hoechst 144
CAS号 : 107254-86-4
货号 : A336852
分子式 : C16H16N2O4
纯度 : 99%+
分子量 : 300.309
MDL号 : MFCD00153851
存储条件:

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

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 105 mg/mL(349.64 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
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 ... 展开 >> Many Locations, Poland 收起 <<
NCT00586027 - Completed - Germany ... 展开 >> Klinikum der Stadt Ludwigshafen, Department of Anesthesiology and Intensive Care Medicine Ludwigshafen, Germany, 67063 收起 <<
NCT02792452 - Recruiting July 2018 United Kingdom ... 展开 >> 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 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.33mL

0.67mL

0.33mL

16.65mL

3.33mL

1.66mL

33.30mL

6.66mL

3.33mL

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