G7798
GYKI-53655 hydrate
>99.0% (HPLC)
别名:
1-(4-aminophenyl)-3-methylcarbamyl-4-methyl-3,4-dihydro-7,8-methylenedioxy-5H-2,3-benzodiazepine hydrochloride, 5-(4-Aminophenyl)-8,9-dihydro-N,8-dimethyl-7H-1,3-dioxolo[4,5-h][2,3]benzodiazepine-7-carboxamide hydrochloride, LY300168 hydrochloride hydrate
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所有图片(1)
About This Item
经验公式(希尔记法):
C19H20N4O3 · HCl · xH2O
CAS号:
分子量:
388.85 (anhydrous basis)
MDL编号:
UNSPSC代码:
12352200
NACRES:
NA.77
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方案
>99.0% (HPLC)
表单
powder
颜色
yellow to orange
溶解性
H2O: >10 mg/mL
储存温度
2-8°C
SMILES字符串
[Cl-].N1(N=C(c3c(cc4c(c3)OCO4)CC1C)c2ccc(cc2)N)C(=O)NC.[H+]
InChI
1S/C19H20N4O3.ClH/c1-11-7-13-8-16-17(26-10-25-16)9-15(13)18(22-23(11)19(24)21-2)12-3-5-14(20)6-4-12;/h3-6,8-9,11H,7,10,20H2,1-2H3,(H,21,24);1H
InChI key
ASLCSBBDVWPSQT-UHFFFAOYSA-N
应用
GYKI-53655 hydrate has been used as a calcium-permeable α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor (AMPA) receptor antagonist in single-particle tracking experiments.
生化/生理作用
GYKI-53655 also inhibits the kainate GluK3 homomeric and GluK2/3 heteromeric receptors. It exhibits anti-ischemic, anti-convulsant, and acute neuroprotective activity.
GYKI-53655 is an AMPA antagonist and noncompetitive negative allosteric modulator.
特点和优势
This compound is featured on the Glutamate Receptors (Ion Channel Family) page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
警示用语:
Danger
危险声明
危险分类
Acute Tox. 3 Oral
储存分类代码
6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
WGK
WGK 1
闪点(°F)
Not applicable
闪点(°C)
Not applicable
T Szabados et al.
Brain research bulletin, 55(3), 387-391 (2001-08-08)
GYKI 52466 [1-(4-aminophenyl)-4-methyl-7,8-methylenedioxy-5H-2,3-benzodiazepine], a non-competitive AMPA [alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionate] and kainate receptor antagonist and its two analogues, GYKI 53405 [1-(4-aminophenyl)-3-acetyl-4-methyl-3,4-dihydro-7,8-methylenedioxy-5H-2,3-benzodiazepine] and GYKI 53655 [1-(4-aminophenyl)-3-methylcarbamyl-4-methyl-3,4-dihydro-7,8-methylenedioxy-5H-2,3-benzodiazepine] were investigated in two seizure models and in MgCl2 induced global cerebral ischaemia, as an acute neuroprotective model.
David Perrais et al.
Neuropharmacology, 56(1), 131-140 (2008-09-02)
A number of kainate receptor antagonists have shown selectivity for receptors containing the GluK1 subunit. Here, we analyze the effects of these GluK1 antagonists on currents mediated by recombinant homomeric GluK3 and heteromeric GluK2/3 receptors expressed in HEK 293 cells
Alice Polenghi et al.
Cell reports, 31(10), 107735-107735 (2020-06-11)
Kainate receptors (KARs) mediate postsynaptic currents with a key impact on neuronal excitability. However, the molecular determinants controlling KAR postsynaptic localization and stabilization are poorly understood. Here, we exploit optogenetic and single-particle tracking approaches to study the role of KAR
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