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- 2025年11月20日
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- 详细信息
- 技术资料
- 供应商：
上海再康生物科技有限公司
- 库存：
大量
- 靶点：
见官方网站
- 级别：
高
- 目录编号：
G-220
- 克隆性：
多克隆
- 抗原来源：
Synthetic
- 保质期：
6个月
- 抗体英文名：
GYKI 53655 hydrochloride
- 抗体名：
GYKI 53655 hydrochloride
- 标记物：
见官方网站
- 宿主：
Synthetic
- 适应物种：
见官方网站
- 免疫原：
见官方网站
- 亚型：
见官方网站
- 形态：
液体或冻干粉
- 应用范围：
见官方网站
- 浓度：
见官方网站
- 保存条件：
-20°C
- 规格：
5 mg, 10 mg, 25 mg, 50 mg
GYKI 53655 hydrochloride
An Antagonist of AMPA and Kainate ReceptorsCat #: G-220
Sizes: 5 mg, 10 mg, 25 mg, 50 mg
Source: Synthetic
MW: 388.85 Da.
Target: AMPA, Kainate receptors
CLICK HERE TO RECEIVE A 5 mg FREE TRIAL SAMPLE!
GYKI 53655 hydrochloride, a racemic 2,3-benzodiazepine is a AMPA and Kainate receptor antagonist. It acts as a non-competitive antagonist and negative allosteric modulator of AMPA receptors and is selective over Kainate receptors. It inhibits AMPA mediated responses in recombinant human GluA1 receptors expressed in HEK293 cells with an approximate IC50 values of 6 µM, and in recombinant human GluA4 expressing cells with an approximate IC50 values of 5 µM1. GYKI 53655 have been reported to be therapeutically effective in several animal models of epilepsy and global brain ischaemia1.
The ionotropic glutamate AMPA receptors (AMPARs) are the primary receptors that mediate fast excitatory synaptic transmission in the mammalian brain. This function is essential for synaptic plasticity, learning, and memory1,2.
Kainate receptors are highly expressed in the developing brain, where they are tonically activated to modulate synaptic transmission, network excitability, and synaptogenesis3.
Alomone Labs is pleased to offer GYKI 53655 hydrochloride (#G-220).
GYKI 53655 hydrochlorideReferences
- Chizh, B.A. et al. (1994) Br. J. Pharmacol. 112, 843.
- Chizh, B.A. et al. (1994) Br. J. Pharmacol. 112, 843.
- Orav, E. et al. (2017) eNeuro 4, 3.
- Our Bioassay
- Specifications
- Related Products
Alomone Labs GYKI 53655 hydrochloride inhibits GluA1 channels expressed in Xenopus oocytes.
Representative time course of GluA1 current, activated by a continuous application (top dotted line) of 1 µM (S)-AMPA (#A-267), and reversibly inhibited by 50 µM GYKI 53655 hydrochloride (#G-220), as indicated (bar), at a holding potential of -80 mV.
Purity>99%.
Effective concentration0.1-100 µM.
Chemical name5-(4-aminophenyl)-N,8-dimethyl-8,9-dihydro-[1,3]dioxolo[4,5-h][2,3]benzodiazepine-7-carboxamide;hydrochloride.
Molecular formulaC19H21ClN4O3.
CAS number143692-48-2.
ActivityGYKI 53655 hydrochloride, an analogue of GYKI 52466 hydrochloride (#G-125), is a non-competitive antagonist and negative allosteric modulator of AMPA receptors (GluR1 IC50 = 5.9 µM)1, selective over Kainate receptors (GluK3 IC50 = 63 µM)2. Exhibits anticonvulsant and neuroprotective activity both in vitro and in vivo3.
Storage before reconstitutionThe product should be stored desiccated at 4°C.
ReconstitutionSoluble up to 100 mM in DMSO or water. Centrifuge all products before handling (10000 x g 5 min).
Storage after reconstitution
Up to four weeks at 4°C or three months at -20°C.
It is recommended to aliquot stock solutions to prevent repeated thawing.
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