Home >> Research Area >>Membrane Transporter/Ion Channel>>AMPAR>> GYKI 53655 hydrochloride

GYKI 53655 hydrochloride

CAS# 143692-48-2

GYKI 53655 hydrochloride

Catalog No. BCC7407----Order now to get a substantial discount!

Product Name & Size Price Stock
GYKI 53655 hydrochloride: 5mg $115 In Stock
GYKI 53655 hydrochloride: 10mg Please Inquire In Stock
GYKI 53655 hydrochloride: 20mg Please Inquire Please Inquire
GYKI 53655 hydrochloride: 50mg Please Inquire Please Inquire
GYKI 53655 hydrochloride: 100mg Please Inquire Please Inquire
GYKI 53655 hydrochloride: 200mg Please Inquire Please Inquire
GYKI 53655 hydrochloride: 500mg Please Inquire Please Inquire
GYKI 53655 hydrochloride: 1000mg Please Inquire Please Inquire
Related Products

Quality Control of GYKI 53655 hydrochloride

Number of papers citing our products

Chemical structure

GYKI 53655 hydrochloride

3D structure

Chemical Properties of GYKI 53655 hydrochloride

Cas No. 143692-48-2 SDF Download SDF
PubChem ID 126757 Appearance Powder
Formula C19H21ClN4O3 M.Wt 388.85
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 100 mM in water and to 100 mM in DMSO
Chemical Name 5-(4-aminophenyl)-N,8-dimethyl-8,9-dihydro-[1,3]dioxolo[4,5-h][2,3]benzodiazepine-7-carboxamide;hydrochloride
SMILES CC1CC2=CC3=C(C=C2C(=NN1C(=O)NC)C4=CC=C(C=C4)N)OCO3.Cl
Standard InChIKey ASLCSBBDVWPSQT-UHFFFAOYSA-N
Standard InChI 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
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of GYKI 53655 hydrochloride

DescriptionNon-competitive AMPA and kainate receptor antagonist. Analog of GYKI 52466. Prolongs the survival time after MgCl2- induced global cerebral ischemia. Exhibits anticonvulsant activity. Also blocks GluK3 homomeric receptors (IC50 = 63 μM) and GluK2b(R)/GluK3 heteroreceptors (IC50 = 32 μM) at high concentrations.

GYKI 53655 hydrochloride Dilution Calculator

Concentration (start)
x
Volume (start)
=
Concentration (final)
x
Volume (final)
 
 
 
C1
V1
C2
V2

calculate

GYKI 53655 hydrochloride Molarity Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
g/mol

calculate

Preparing Stock Solutions of GYKI 53655 hydrochloride

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.5717 mL 12.8584 mL 25.7169 mL 51.4337 mL 64.2921 mL
5 mM 0.5143 mL 2.5717 mL 5.1434 mL 10.2867 mL 12.8584 mL
10 mM 0.2572 mL 1.2858 mL 2.5717 mL 5.1434 mL 6.4292 mL
50 mM 0.0514 mL 0.2572 mL 0.5143 mL 1.0287 mL 1.2858 mL
100 mM 0.0257 mL 0.1286 mL 0.2572 mL 0.5143 mL 0.6429 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

Organizitions Citing Our Products recently

 
 
 

Calcutta University

University of Minnesota

University of Maryland School of Medicine

University of Illinois at Chicago

The Ohio State University

University of Zurich

Harvard University

Colorado State University

Auburn University

Yale University

Worcester Polytechnic Institute

Washington State University

Stanford University

University of Leipzig

Universidade da Beira Interior

The Institute of Cancer Research

Heidelberg University

University of Amsterdam

University of Auckland
TsingHua University
TsingHua University
The University of Michigan
The University of Michigan
Miami University
Miami University
DRURY University
DRURY University
Jilin University
Jilin University
Fudan University
Fudan University
Wuhan University
Wuhan University
Sun Yat-sen University
Sun Yat-sen University
Universite de Paris
Universite de Paris
Deemed University
Deemed University
Auckland University
Auckland University
The University of Tokyo
The University of Tokyo
Korea University
Korea University
Featured Products
New Products
 

References on GYKI 53655 hydrochloride

Antagonism of recombinant and native GluK3-containing kainate receptors.[Pubmed:18761361]

Neuropharmacology. 2009 Jan;56(1):131-40.

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 and activated by fast application of glutamate. We show that, amongst these compounds, UBP302, UBP310 and UBP316 effectively block recombinant homomeric GluK3 receptors. However, these antagonists are ineffective in blocking homomeric GluK2 or heteromeric GluK2/3 receptors. In addition, these antagonists do not affect presynaptic kainate receptors at mouse hippocampal mossy fibre synapses, which are thought to be composed of GluK2 and GluK3 subunits. Moreover, the AMPA receptor-selective non-competitive antagonist GYKI 53655 blocks, at high concentrations, GluK3-containing receptors and decreases short-term plasticity at mossy fibre synapses. These results expand the range of targets of kainate receptor antagonists and provide pharmacological tools to study the elusive mechanisms of neurotransmitter control by presynaptic kainate receptors.

Comparison of anticonvulsive and acute neuroprotective activity of three 2,3-benzodiazepine compounds, GYKI 52466, GYKI 53405, and GYKI 53655.[Pubmed:11489346]

Brain Res Bull. 2001 Jun;55(3):387-91.

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-benzod iazepine] 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. The ED(50) values of GYKI 52466 for suppression of the tonic and clonic phases of sound-induced seizures were 3.6 and 4.3 mg/kg, respectively. The corresponding data for GYKI 53405 were 1.1 and 3.1 mg/kg, while ED(50) values of GYKI 53655 were 1.3 and 2.0 mg/kg, respectively. The inhibition of seizure evoked by maximal electroshock was also found to be remarkable: the ED(50) values of GYKI 52466 and its two analogues were 6.9, 2.6, and 2.2 mg/kg, respectively. All compounds prolonged the survival times in MgCl2 induced global cerebral ischaemia test in a dose-dependent fashion, with PD(50) (dose of 50% prolongation) values of 24.1, 8.3, and 8.2 mg/kg intraperitoneal, respectively. In audiogenic seizure model the duration of anticonvulsant action of 10 mg/kg GYKI 52466 and 5 mg/kg GYKI 53405, GYKI 53655 were examined, too. The effect of GYKI 52466 decreased to 50% after 2 h, while the analogues showed more than 80% seizure suppression 3 h after treatment. After 6 h the effect of GYKI 53655 decreased to zero, while the effect of GYKI 52466, remained on the 50% level.

Selective antagonism of AMPA receptors unmasks kainate receptor-mediated responses in hippocampal neurons.[Pubmed:7826635]

Neuron. 1995 Jan;14(1):185-9.

Although both protein and mRNAs for kainate receptor subunits are abundant in several brain regions, the responsiveness of AMPA receptors to kainate has made it difficult to demonstrate the presence of functional kainate-type receptors in native cells. Recently, however, we have shown that many hippocampal neurons in culture express glutamate receptors of the kainate type. The large nondesensitizing response that kainate induces at AMPA receptors precludes detection and analysis of smaller, rapidly desensitizing currents induced by kainate at kainate receptors. Consequently, the functional significance of these strongly desensitizing glutamate receptors remains enigmatic. We report here that the family of new noncompetitive antagonists of AMPA receptors (GYKI 52466 and 53655) minimally affects kainate-induced responses at kainate receptors while completely blocking AMPA receptor-mediated currents, making it possible to separate the responses mediated by each receptor. These compounds will allow determination of the role played by kainate receptors in synaptic transmission and plasticity in the mammalian brain, as well as evaluation of their involvement in neurotoxicity.

Description

GYKI53655 hydrochloride is an α-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA) antagonist.

Keywords:

GYKI 53655 hydrochloride,143692-48-2,Natural Products,AMPAR, buy GYKI 53655 hydrochloride , GYKI 53655 hydrochloride supplier , purchase GYKI 53655 hydrochloride , GYKI 53655 hydrochloride cost , GYKI 53655 hydrochloride manufacturer , order GYKI 53655 hydrochloride , high purity GYKI 53655 hydrochloride

Online Inquiry for:

      Fill out the information below

      • Size:Qty: - +

      * Required Fields

                                      Result: