NPPB
(Synonyms: 5-硝基-2-(3-苯丙胺)苯甲酸) 目录号 : GC14268
A chloride channel blocker and GPR35 agonist
Cas No.:107254-86-4
Sample solution is provided at 25 µL, 10mM.
NPPB, 5-nitro-2-(3-phenylpropylamino)-benzoic acid, is a potent inhibitor of chloride channel with IC50 of 80 nM for the short circuit current.[1]
Chloride channel blockers possess several sites of interaction, including the negatively charged carboxylate group, the secondary amine group which probably carries a positive partial charge, and for the very potent agents like NPPB an additional negative partial charge at the -NO2 substituent. In addition, an apolar interaction with a cycloaryl residue is necessary, and this site of interaction has a specific spacing from the secondary amino nitrogen.[1]
NPPB was evaluated for the activity on the equivalent short circuit current, corresponding to the secondary active transport of Cl- and measurements of the voltage across the basolateral membrane. The result revealed that NPPB possessed a good potency with IC50 of 80 nM for inhibiting the short circuit current. Furthermore, NPPB was also tested for its activity on various anion channels. Adopting freshly-isolated cells from the rat portal vein, the effects of NPPB were investigated on evoked and spontaneous currents by use of conventional whole-cell recording and perforated-patch techniques. At a holding potential of -60 mV in potassium-free, caesium-containing solutions, NPPB (10 μM) inhibited Ca-sensitive chloride currents (ICI(Ca)) evoked by caffeine (10 mM) and by noradrenaline (10μM) by the extend of 58% and 96%, respectively. In addition, at a holding potential of -2 mV in potassium -containing solutions, NPPB (10 μM) inhibited charybdotoxin-sensitive potassium-currents (IBK(Ca)) induced by noradrenaline (10 μM) and acetylcholine (10 μM) by approximately 90%. NPPB's inhibitory effects of volume-activated taurine, glucose, and uridine influxes was studied. The IC50 for the inhibition of the volume- activated fluxes by NPPB was around 12 μM. [1-3]
References:
[1] Wangemann, Ph, et al. "Cl−-channel blockers in the thick ascending limb of the loop of Henle Structure activity relationship." Pflügers Archiv 407.2 (1986): S128-S141.
[2] Kirkup, A. J., G. Edwards, and A. H. Weston. "Investigation of the effects of 5‐nitro‐2‐(3‐phenylpropylamino)‐benzoic acid (NPPB) on membrane currents in rat portal vein." British journal of pharmacology 117.1 (1996): 175-183.
[3] Kirk, Kiaran, J. C. Ellory, and J. D. Young. "Transport of organic substrates via a volume-activated channel." Journal of Biological Chemistry 267.33 (1992): 23475-23478.
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Cell experiment: |
Cells are seeded in the 96-well microtiter plate at a density of 5×103 cells per well and incubated at 37°C for 24 h in a humidified 5% CO2 atmosphere. After removing the culture medium, fresh media containing various concentrations of NPPB is added, and incubated for 24 h. Next, 100 μL of Thiazolyl blue tetrazolium bromide at 0.5 mg/mL is added to each well and incubated at 37°C for 1 h. Cells are then dissolved in 100 μL of DMSO, and the absorbance is measured at 570 nm with a Microplate Reader. Concentration-response curves of NPPB are fitted to a Hill equation to obtain GI50 and GI80 (50% and 80% growth inhibition concentrations, respectively) values[2]. |
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References: [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. |
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| Cas No. | 107254-86-4 | SDF | |
| 别名 | 5-硝基-2-(3-苯丙胺)苯甲酸 | ||
| 化学名 | 5-nitro-2-((3-phenylpropyl)amino)benzoic acid | ||
| Canonical SMILES | OC(C1=CC([N+]([O-])=O)=CC=C1NCCCC2=CC=CC=C2)=O | ||
| 分子式 | C16H16N2O4 | 分子量 | 300.31 |
| 溶解度 | ≥ 11.05mg/mL in DMSO | 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 | 3.3299 mL | 16.6495 mL | 33.2989 mL |
| 5 mM | 0.666 mL | 3.3299 mL | 6.6598 mL |
| 10 mM | 0.333 mL | 1.6649 mL | 3.3299 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。
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet