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GTS-21二盐酸盐(DMBX-A)

GTS-21二盐酸盐(DMBX-A)

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?GTS-21二盐酸盐(DMBX-A)名称


















中文名

(1:2),(3E)-3-[(2,4-二甲氧基苯基)亚甲基]-3,4,5,6-四氢-2,3-联吡啶盐酸盐
英文名

3-(2,4-Dimethoxy-benzyl)-3,4,5,6-tetrahydro-[2,3']bipyridinyl
中文别名


(3E)-3-[(2,4-二甲氧基苯基)亚甲基]-3,4,5,6-四氢-2,3′-联吡啶二盐酸盐



英文别名
更多





?GTS-21二盐酸盐(DMBX-A)生物活性












































描述
GTS-21二盐酸盐是一种选择性α7烟碱型乙酰胆碱受体 (α7nAChR) 激动剂。
相关类别




溶解度

体外:

DMSO:16.5 mg / mL(43.27 mM;需要超声波和加热)


储备液

1 mM 2.6226 mL 13.1130 mL 26.2261 mL
5 mM 0.5245 mL 2.6226 mL 5.2452 mL
10 mM 0.2623 mL 1.3113 mL 2.6226 mL


存储

粉末 -20℃下 3年
4℃下 2年
在溶剂中 -80℃下 6个月
-20℃下 1个月


运输

室温;可能会有所不同
SMILES

COC1=CC(OC)=CC=C1/C=C2CCCN=C2C3=CC=CN=C3.Cl[H].Cl[H]
参考文献

[1]. Yue Y, et al. GTS-21 attenuates lipopolysaccharide-induced inflammatory cytokine production in vitro by modulating the Akt and NF-κB signaling pathway through the α7 nicotinic acetylcholine receptor. Int Immunopharmacol. 2015 Dec;29(2):504-12.

[2]. Nullens S, et al. EFFECT OF GTS-21, AN ALPHA7 NICOTINIC ACETYLCHOLINE RECEPTOR AGONIST, ON CLP-INDUCED INFLAMMATORY, GASTROINTESTINAL MOTILITY, AND COLONIC PERMEABILITY CHANGES IN MICE. Shock. 2016 Apr;45(4):450-9.


相关活性
小分子




PNU-282987



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卡巴胆碱



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柠檬酸柠康碱(MLA)



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Monepantel



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六甲溴铵



|

N-(5-氯-2,4-二甲氧基苯基)-N’-(5-甲基-3-异唑基)脲



|

盐酸甲氯芬酯



|

ZSET1446



|

阿尼西坦



|

Desformylflustrabromine hydrochloride



|

Encenicline hydrochloride



|

盐酸洛贝林



|

Tebanicline hydrochloride



|

伐尼克兰



|

长春质碱






?GTS-21二盐酸盐(DMBX-A)物理化学性质











































密度 1.1±0.1 g/cm3
沸点 485.6±45.0 °C at 760 mmHg
熔点 216-217℃ (decomposition)
分子式 C19H22Cl2N2O2
分子量 381.30
闪点 247.5±28.7 °C
PSA 43.71000
LogP 2.64
外观性状 powder,faint yellow to dark yellow
蒸汽压 0.0±1.2 mmHg at 25°C
折射率 1.580
储存条件 2-8°C
水溶解性 H2O: >5mg/mL






?GTS-21二盐酸盐(DMBX-A)安全信息






















危险品运输编码 NONH for all modes of transport
WGK德国 3
RTECS号 DW1764860
海关编码 2933399090











?GTS-21二盐酸盐(DMBX-A)海关















海关编码 2933399090
中文概述 2933399090. 其他结构含非稠合吡啶环的化合物. 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, 乌洛托品请注明外观, 6-己内酰胺请注明外观, 签约日期
Summary 2933399090. other compounds containing an unfused pyridine ring (whether or not hydrogenated) in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%








?GTS-21二盐酸盐(DMBX-A)文献28

更多文献














Central muscarinic cholinergic activation alters interaction between splenic dendritic cell and CD4+CD25- T cells in experimental colitis.

PLoS ONE 9(10) , e109272, (2014)

The cholinergic anti-inflammatory pathway (CAP) is based on vagus nerve (VN) activity that regulates macrophage and dendritic cell responses in the spleen through alpha-7 nicotinic acetylcholine recep…





Pro-cognitive activity in rats of 3-furan-2-yl-N-p-tolyl-acrylamide, a positive allosteric modulator of the α7 nicotinic acetylcholine receptor.

Br. J. Pharmacol. 172 , 5123-35, (2015)

α7 nicotinic acetylcholine receptors (α7 nAChRs) may represent useful targets for cognitive improvement. The aim of this study is to compare the pro-cognitive activity of selective α7-nAChR ligands, i…





The α7 nicotinic acetylcholine receptor ligands methyllycaconitine, NS6740 and GTS-21 reduce lipopolysaccharide-induced TNF-α release from microglia.

J. Neuroimmunol. 251(1-2) , 65-72, (2012)

The anti-inflammatory properties of, particularly the α7, nicotinic acetylcholine receptors (nAChRs) in the peripheral immune system are well documented. There are also reports of anti-inflammatory ac…









?GTS-21二盐酸盐(DMBX-A)英文别名










































3-(2,4-Dimethoxy-benzyl)-3,4,5,6-tetrahydro-[2,3']bipyridinyl


3-[(3E)-3-[(2,4-dimethoxyphenyl)methylidene]-5,6-dihydro-4H-pyridin-2-yl]pyridine dihydrochloride


3-(2,4-dimethoxybenzylidene)anabaseine


2,3′-Bipyridine, 3-[(2,4-dimethoxyphenyl)methylene]-3,4,5,6-tetrahydro-, (3E)-


3-(2,4-Dimethoxybenzyl)-3,4,5,6-tetrahydro-2,3′-bipyridine


(3E)-3-(2,4-Dimethoxybenzylidene)-3,4,5,6-tetrahydro-2,3′-bipyridine


3-(2,4)-DiMethoxybenzylidineanabaseine


GTS-21


DMXB-A


GTS 21 2HCl


GTS-21 (dihydrochloride)








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