| Field | Specification |
|---|---|
| Mfr No | |
| Activity | |
| Cas No. | |
| Concentration | |
| Form | Lyophilized powder. |
| Product Type | |
| Purity | |
| Reconstitution | |
| Shipping | |
| Solubility | Soluble up to 100 mM in DMSO or water. Centrifuge all products before handling (10000 x g 5 min). |
| Source | Synthetic |
| Storage | |
| Target |
Product details
- Chemical name: 5-(4-aminophenyl)-N,8-dimethyl-8,9-dihydro-[1,3]dioxolo[4,5-h][2,3]benzodiazepine-7-carboxamide;hydrochloride.
- CAS number: 143692-48-2
- Molecular formula: C19H21ClN4O3.
- Purity: >99% (HPLC)
- Concentration: 0.1-100 µM.
- Form: Lyophilized powder.
- Solubility: Soluble up to 100 mM in DMSO or water. Centrifuge all products before handling (10000 x g 5 min).
- Reconstitution: Soluble up to 100 mM in DMSO or water. Centrifuge all products before handling (10000 x g 5 min).
- Shipping: Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
- Target: AMPA, Kainate receptors
- Source: Synthetic
- Activity: GYKI 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.
Scientific background
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.
Lead time: 1-2 Business Days
Country of origin: Israel/IL
Applications key
Application key: FC- Flow cytometry, IFC- Indirect flow cytometry, IHC- Immunohistochemistry,LCI- Live cell imaging, Calcium imaging assay,Cell survival assay, Electrophysiology, Neurite outgrowth assay.
Bioassay tested: Yes
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