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PNU-120596

PNU-120596

产品编号 T6950   CAS 501925-31-1
别名: NSC 216666

PNU-120596 (NSC-216666) 是一种选择性α7 nAChR 阳性变构调节剂,EC50为 216 nM,可用于精神病和神经疾病的研究。

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PNU-120596 Chemical Structure
PNU-120596, CAS 501925-31-1
规格 价格/CNY 货期 数量
5 mg ¥ 273 现货
10 mg ¥ 462 现货
25 mg ¥ 888 现货
50 mg ¥ 1,680 现货
100 mg ¥ 2,950 现货
200 mg ¥ 4,260 现货
1 mL * 10 mM (in DMSO) ¥ 273 现货
产品目录号及名称: PNU-120596 (T6950)
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 PNU-120596 (NSC-216666) is a positive allosteric modulator of α7 nAChR with EC50 of 216 nM.
靶点活性 α7 nAChR:NA
体外活性 PNU-120596 increases agonist (Ach)-evoked calcium flux mediated by an engineered variant of the human α7 nAChR. PNU-120596 increases agonists (choline and ACh)-evoked currents mediated by wild-type receptors and also demonstrates a pronounced prolongation of the evoked response in the continued presence of agonist in Xenopus oocytes. PNU-120596 increases the channel mean open time ofα7 nAChRs but has no effect on ion selectivity and relatively little, if any, effect on unitary conductance. When applied to acute hippocampal slices, PNU-120596 increases the frequency of ACh-evoked GABAergic postsynaptic currents measured in pyramidal neurons; this effect is suppressed by TTX, suggesting that PNU-120596 modulates the function of α7 nAChRs located on the somatodendritic membrane of hippocampal interneurons. [1] Besides the positive modulation to α7 nAChR, PNU-120596 induces a profound retardation of the kinetics of desensitization, raising the potential of Ca2+-induced toxicity through excessive stimulation of α7 nAChR. [2] PNU-120596 causes changes in cysteine accessibility at the inner beta sheet, transition zone and agonist binding site while binding to α7 nAChR. Binding sites for PNU-120596 are not in the agonist-binding sites and PNU-120596 enhances agonist-evoked gating of nicotinic receptors by eliciting conformational effects that are similar but nonidentical to the gating conformations promoted by Ach. [3]
体内活性 Systemic administration of PNU-120596 (1 mg/kg) to rats improves the auditory gating deficit caused by amphetamine, a model proposed to reflect a circuit level disturbance associated with schizophrenia. [1] When administered prior to Carrageenan, 30 mg/kg PNU-1230596 significantly blunts mechanical hyperalgesia and weight bearing deficits for up to 4 hours. PNU-120596 attenuates the carrageenan-induced increase in levels of TNF-α and IL-6 within the hindpaw oedema, diclofenac only attenuated IL-6 levels. Established mechanical hyperalgesia induced by Carrageenan or CFA is also partially reversed by PNU-120596. [4]
激酶实验 Ca2+ Fluorescence Assay: SH-EP1 human epithelial cells expressing a variant of theα7 nAChR (α7*) are grown in minimal essential medium (MEM) containing nonessential amino acids supplemented with 10% fetal bovine serum, L-glutamine, 100 U/ml penicillin/streptomycin, 250 ng/mL fungizone, 400 μg/mL hygromycin B, and 800 μg/mL geneticin. α7* is a variant of the human α7 nAChR, with two point mutations in the first transmembrane domain (T230P and C241S) that allow for high functional expression in SH-EP1 cells [Groppi VE, Wolfe ML, Berkenpas MB (2003) U.S. Patent 6,693,172 B1]. Cells are grown in a 37 °C incubator with 6% CO2. Cells are trypsinized and plated in 96-well plates with dark side walls and clear bottoms at a density of 2 × 104 cells/well 2 days before analysis. Cells are loaded with a mixture of Calcium reen-1AM in anhydrous dimethylsulfoxide and 20% pluronic F-127. This reagent is added directly to the growth medium of each well to achieve a final concentration of 2 μM Calcium Green-1 AM. Cells are then incubated in the dye for 1 hour at 37 °C and then washed four times with Mark's modified Earle's balanced salt solution (MMEBSS) composed of the following (inmM): 4 CaCl2, 0.8 MgSO4, 20 NaCl, 5.3 KCl, 5.6 D-glucose, 20 Tris-HEPES, and 120 N-methyl-D-glucamine, pH 7.4. After the fourth cycle, the cells are allowed to incubate at 37 °C for at least 10 minutes. The final volume of MMEBSS in each well is 100 μL and atropine is added to all wells for a final concentration of 1 μM. A fluorometric imaging plate reader (FLIPR; Molecular Devices, Union City, CA) is set up to excite Calcium Green at 488 nm using 500 mW of power and reading fluorescence emission of >525 nm. A 0.5 seconds exposure is used to illuminate each well. Fluorescence is detected using an F-stop set of either 2.0 or 1.2. After 30 seconds of baseline recording, test compounds are added to each well of a 96-well plate in 50 μL of a 3 × stock.In each experiment, four wells are used as vehicle (0.2% DMSO) controls.
细胞实验 SH-SY5Y-α7 cells are plated on 96-well plates at a density of 15,000 cells per well (100 μL of 1.5 × 105 cells per mL) in complete growth medium and placed into a 37 °C incubator for 20 to 24 hours. Complete growth medium then is replaced with experimental medium alone ("PNU-120596 free") or containing appropriate concentrations of PNU-120596 and returns to the 37 °C ncubator for 20 to 24 hours. The medium is then replaced with fresh experimental medium and 20 μL per well MTS solution and returned to the 37 °C incubator for 3 hours, after which the plate is read on a microplate spectrophotometer at an absorbance of 490 nm. For all data analysis, data are normalized to untreated compound-free wells (100% cell viability) and a background absorbance taken from wells containing experimental medium and MTS solution.(Only for Reference)
动物实验 Animal Models: male Sprague Dawley rats (weighing 250–300 g)Formulation: PNU-120596 is dissolved in 5% DMSO and 5% Solutol in PBS.Dosages: 1 mg/kgAdministration: PNU-120596 is intravenously administrated 5 minutes before auditory gating measurements.
别名 NSC 216666
分子量 311.72
分子式 C13H14ClN3O4
CAS No. 501925-31-1

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 31.2 mg/mL (100 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.208 mL 16.04 mL 32.0801 mL 80.2002 mL
5 mM 0.6416 mL 3.208 mL 6.416 mL 16.04 mL
10 mM 0.3208 mL 1.604 mL 3.208 mL 8.02 mL
20 mM 0.1604 mL 0.802 mL 1.604 mL 4.01 mL
50 mM 0.0642 mL 0.3208 mL 0.6416 mL 1.604 mL
100 mM 0.0321 mL 0.1604 mL 0.3208 mL 0.802 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Hurst RS, et al, J Neurosci, 2005, 25(17), 4396-4405. 2. Ng HJ, et al, Proc Natl Acad Sci USA, 2007, 104(19), 8059-8064. 3. Barron SC, et al, Mol Pharmacol, 2009 76(2), 253-263. 4. Munro G, et al, Br J Pharmacol, 2012, doi: 10.1111/j.1476-5381.2012.02003.x
Amitriptyline hydrochloride Chlorprothixene hydrochloride M4 mAChR agonist-1  NS 1738 Levamisole hydrochloride mAChR-IN-1 hydrochloride Nebracetam hydrochloride CHF5407

相关化合物库

该产品包含在如下化合物库中:
神经退行性疾病化合物库 共价抑制剂库 临床前化合物库 NO PAINS 化合物库 神经递质受体化合物库 免疫/炎症分子化合物库 已知活性化合物库 离子通道库 经典已知活性库 神经信号分子库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
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% ddH2O
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技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

PNU-120596 501925-31-1 Neuroscience AChR pain anti-hyperalgesia inhibit inflammatory Nicotinic acetylcholine receptors TNF-α Inhibitor α7nAChR disorders PNU 120596 neurological NSC 216666 NSC216666 IL-6 nAChR PNU120596 NSC-216666 inhibitor

 

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