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Home / Biochemicals / Small Molecules

GYKI 53655 hydrochloride

SKU : BHB21300160

An Antagonist of AMPA and Kainate Receptors

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Mfr.No.	G-220, G-220_10 mg, G-220_25 mg, G-220_5 mg, G-220_50 mg
Description	GYKI 53655 hydrochloride (#G-220) is a highly pure, synthetic, and biologically active compound.
Molecular Formula	C19H21ClN4O3.
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 uM, and in recombinant human GluA4 expressing cells with an approximate IC50 values of 5 uM1. 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.
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
Concentration	0.1-100 uM.
Reconstitution	Soluble up to 100 mM in DMSO or water. Centrifuge all products before handling (10000 x g 5 min).
Cas Number	143692-48-2
Molecular Weight	388.85
Solubility	Soluble up to 100 mM in DMSO or water. Centrifuge all products before handling (10000 x g 5 min).
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 uM)1, selective over Kainate receptors (GluK3 IC50 = 63 uM)2. Exhibits anticonvulsant and neuroprotective activity both in vitro and in vivo3.
Country Of Origin	Israel/IL
UNSPSC Code	41116134
Application	FC- Flow cytometry, IFC- Indirect flow cytometry, IHC- Immunohistochemistry,LCI- Live cell imaging, Calcium imaging assay,Cell survival assay, Electrophysiology, Neurite outgrowth assay
Lead Time	1-2 Business Days
Notes	Bioassay Tested: Yes Chemical Name: 5-(4-aminophenyl)-N,8-dimethyl-8,9-dihydro-(1,3)dioxolo(4,5-h)(2,3)benzodiazepine-7-carboxamide;hydrochloride.

Purity	>99% (HPLC)
Form	Lyophilized powder.
Storage	Storage After Reconstitution: The reconstituted solution can be stored at 4°C for up to 1 week. For longer periods (up to 6 months), small aliquots should be stored at -20°C. We do not recommend storing the product in working solutions for longer than a few days. Avoid multiple freeze-thaw cycles. Storage of solutions: Up to four weeks at 4°C or three months at -20°C.It is recommended to aliquot stock solutions to prevent repeated thawing.

Product Manual	SDS

Reference	Chizh, B.A. et al. (1994) Br. J. Pharmacol. 112, 843. Orav, E. et al. (2017) eNeuro 4, 3. Bleakman, D. et al. (1996) Neuropharmacology 35,1689. Perrais, D. et al. (2009) Neuropharmacology 56, 131. Szabados, T. et al. (2001) Brain. Res. Bull. 55, 387.

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Combination SKU	Supplier No.	Size	Your price	Quantity
BHB21300160-1	G-220_10 mg	10 mg	$325		Add to Cart
BHB21300160-2	G-220_25 mg	25 mg	$652		Add to Cart
BHB21300160-3	G-220_5 mg	5 mg	$266		Add to Cart
BHB21300160-4	G-220_50 mg	50 mg	$1172		Add to Cart

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