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N-(5-氯-2,4-二甲氧基苯基)-N’-(5-甲基-3-异唑基)脲

用途

PNU-120596 (NSC 216666)是α7 nAChR正向变构调节剂,EC50为0.2 μM。

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名称

[ CAS 号 ]:
501925-31-1

[ 中文名 ]:
N-(5-氯-2,4-二甲氧基苯基)-N’-(5-甲基-3-异唑基)脲

[ 英文名 ]:
PNU-120596

[中文别名 ]:

[英文别名 ]:

PNU-120596
PNU120596

生物活性

[ 描述 ]:

PNU-120596 (NSC 216666)是α7 nAChR正向变构调节剂,EC50为0.2 μM。

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> 胆碱受体

信号通路 >> 神经信号通路 >> 胆碱受体

研究领域 >> 神经疾病

[参考文献]

[1]. Hurst RS, et al. A novel positive allosteric modulator of the alpha7 neuronal nicotinic acetylcholine receptor: in vitro and in vivo characterization. J Neurosci, 2005, 25(17), 4396-4405.

[2]. Ng HJ, et al. Nootropic alpha7 nicotinic receptor allosteric modulator derived from GABAA receptor modulators. Proc Natl Acad Sci USA, 2007, 104(19), 8059-8064.

[3]. Barron SC, et al. An allosteric modulator of alpha7 nicotinic receptors, N-(5-Chloro-2,4-dimethoxyphenyl)-N'-(5-methyl-3-isoxazolyl)-urea (PNU-120596), causes conformational changes in the extracellular ligand binding domain similar to those caused by ace

[4]. Munro G, et al. The α7 nicotinic ACh receptor agonist compound B and positive allosteric modulator PNU-120596 both alleviate inflammatory hyperalgesia and cytokine release in the rat. Br J Pharmacol, 2012, doi: 10.1111/j.1476-5381.2012.02003.x

[相关活性小分子]

物理化学性质

[ 密度 ]:
1.4±0.1 g/cm3

[ 沸点 ]:
385.0±42.0 °C at 760 mmHg

[ 分子式 ]:
C₁₃H₁₄ClN₃O₄

[ 分子量 ]:
311.721

[ 闪点 ]:
186.6±27.9 °C

[ 精确质量 ]:
311.067291

[ PSA ]:
85.62000

[ LogP ]:
2.14

[ 外观性状 ]:
white to off-white

[ 蒸汽压 ]:
0.0±0.9 mmHg at 25°C

[ 折射率 ]:
1.625

[ 储存条件 ]:
Desiccate at +4°C

[ 水溶解性 ]:
DMSO: >10mg/mL

MSDS

详细MSDS(安全技术说明书)

安全信息

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

[ 海关编码 ]:
2934999090

海关

[ 海关编码 ]: 2934999090

[ 中文概述 ]:
2934999090. 其他杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

文献

Activation of Alpha 7 Cholinergic Nicotinic Receptors Reduce Blood-Brain Barrier Permeability following Experimental Traumatic Brain Injury.

J. Neurosci. 36 , 2809-18, (2016)

Traumatic brain injury (TBI) is a major human health concern that has the greatest impact on young men and women. The breakdown of the blood-brain barrier (BBB) is an important pathological consequenc...

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