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Merck
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重要文件

G7798

Sigma-Aldrich

GYKI-53655 hydrate

>99.0% (HPLC)

同義詞:

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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About This Item

經驗公式（希爾表示法）:
C19H20N4O3 · HCl · xH2O
CAS號碼:
143692-48-2
分子量：:
388.85 (anhydrous basis)
MDL號碼:
MFCD01941362
分類程式碼代碼:
12352200
NACRES:
NA.77
暫時無法取得訂價和供貨情況

化驗

>99.0% (HPLC)

形狀

powder

顏色

yellow to orange

溶解度

H2O: >10 mg/mL

儲存溫度

2-8°C

SMILES 字串

[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 密鑰

ASLCSBBDVWPSQT-UHFFFAOYSA-N

應用

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.[1]

生化／生理作用

GYKI-53655 also inhibits the kainate GluK3 homomeric and GluK2/3 heteromeric receptors.[2] It exhibits anti-ischemic, anti-convulsant, and acute neuroprotective activity.[3]
GYKI-53655 is an AMPA antagonist and noncompetitive negative allosteric modulator.

特點和優勢

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.

象形圖

Skull and crossbones
GHS06

訊號詞

Danger

危險聲明

H301

危險分類

Acute Tox. 3 Oral

儲存類別代碼

6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects

水污染物質分類（WGK）

WGK 1

閃點（°F）

Not applicable

閃點（°C）

Not applicable

從最近期的版本中選擇一個：

分析證明 (COA)

Lot/Batch Number
100M4613V
0000012755
0000012756
100M4613

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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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