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NPPB

NPPB用途

NPPB 是外向整流氯化物通道 (ORCC) 的阻断剂。

NPPB名称

[ CAS 号 ]:
107254-86-4

[ 中文名 ]:
5-硝基-2-(3-苯丙胺)苯甲酸

[ 英文名 ]:
NPPB

[英文别名 ]:

5-nitro-2-(3-phenylpropylamino)benzoic acid
MFCD00153851
NPPB

NPPB生物活性

[ 描述 ]:

NPPB 是外向整流氯化物通道 (ORCC) 的阻断剂。

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> 氯离子通道

研究领域 >> 神经疾病

[ 靶点 ]

ORCC[1]

[体外研究]

浴液中的0.1mM NPPB将通道开放概率从0.89±0.06降低到0.11±0.04(n = 5,P <0.01)[1]。用125μMNPPB的50％抑制浓度(IC50)观察到剂量依赖性的氯电流抑制。 NPPB本身也显示出对神经胶质瘤细胞的细胞毒性,GI50约为500μM[2]。

[细胞实验]

将细胞以每孔5×103个细胞的密度接种在96孔微量滴定板中，并在潮湿的5％CO 2气氛中于37℃温育24小时。除去培养基后，加入含有各种浓度NPPB的新鲜培养基，并培养24小时。接下来，向每个孔中加入100μL0.5mg/ mL的噻唑基蓝四唑溴化物，并在37℃下孵育1小时。然后将细胞溶解在100μLDMSO中，用Microplate Reader在570nm处测量吸光度。将NPPB的浓度 - 响应曲线拟合为Hill方程以获得GI50和GI80（分别为50％和80％生长抑制浓度）值[2]。

[参考文献]

[1]. Li J, et al. Enhancement of an outwardly rectifying chloride channel in hippocampal pyramidal neurons after cerebral ischemia. Brain Res. 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 Channel Blocker. ACS Chem Neurosci. 2016 Mar 16;7(3):275-85.

[相关活性小分子]

NPPB物理化学性质

[ 密度 ]:
1.323 g/cm3

[ 沸点 ]:
523.5ºC at 760 mmHg

[ 熔点 ]:
178-179ºC

[ 分子式 ]:
C₁₆H₁₆N₂O₄

[ 分子量 ]:
300.30900

[ 精确质量 ]:
300.11100

[ PSA ]:
95.15000

[ LogP ]:
3.93390

[ 蒸汽压 ]:
8.73E-12mmHg at 25°C

[ 折射率 ]:
1.653

[ 储存条件 ]:
2-8℃

NPPBMSDS

详细MSDS(安全技术说明书)

NPPB安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危险品运输编码 ]:
NONH for all modes of transport

[ 海关编码 ]:
2922499990

NPPB海关

[ 海关编码 ]: 2922499990

[ 中文概述 ]:
2922499990 其他氨基酸及其酯及它们的盐（含有一种以上含氧基的除外）. 增值税率:17.0% 退税率:9.0% 监管条件:AB(入境货物通关单,出境货物通关单) 最惠国关税:6.5% 普通关税:30.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 乙醇胺及其盐应报明色度, 乙醇胺及其盐应报明包装

[ 监管条件 ]: A.入境货物通关单 B.出境货物通关单

[ 检验检疫 ]: P.进境动植物、动植物产品检疫 Q.出境动植物、动植物产品检疫 R.进口食品卫生监督检验 S.出口食品卫生监督检验 M.进口商品检验 N.出口商品检验

[ Summary ]:
HS:2922499990 other amino-acids, other than those containing more than one kind of oxygen function, and their esters; salts thereof VAT:17.0% Tax rebate rate:9.0% Supervision conditions:AB(certificate of inspection for goods inward,certificate of inspection for goods outward) MFN tariff:6.5% General tariff:30.0%

NPPB文献

Ion channel expression in the developing enteric nervous system.

PLoS ONE 10(3) , e0123436, (2015)

The enteric nervous system arises from neural crest-derived cells (ENCCs) that migrate caudally along the embryonic gut. The expression of ion channels by ENCCs in embryonic mice was investigated usin...

Role of anoctamin-1 and bestrophin-1 in spinal nerve ligation-induced neuropathic pain in rats.

Mol. Pain 11 , 41, (2015)

Calcium-activated chloride channels (CaCCs) activation induces membrane depolarization by increasing chloride efflux in primary sensory neurons that can facilitate action potential generation. Previou...

Caspase-dependent cell death-associated release of nucleosome and damage-associated molecular patterns.

Cell Death Dis. 5 , e1494, (2014)

Apoptosis, which is anti-inflammatory, and necrosis, which is pro-inflammatory, represent the extremes of the cell death spectrum. Cell death is complex and both apoptosis and necrosis can be observed...

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