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GYKI53655 hydrochloride

GYKI53655 hydrochloride

Item no.	CS-0025621-5mg
Manufacturer	ChemScene
Amount	5mg
Category	Reagents & Chemicals Molecules
Type	Molecules
Specific against	other
ECLASS 10.1	32169090
ECLASS 11.0	32169090
UNSPSC	12000000
Similar products	143692-48-2
Available
CAS	143692-48-2
Purity	>98%
Formula	C19H21ClN4O3
MWt	388.85
Solubility	H2O : 8 mg/mL (20.57 mM; Need ultrasonic and warming); DMSO : >= 160 mg/mL (411.47 mM)
Clinical Information	No Development Reported
Pathway	Membrane Transporter/Ion Channel; Neuronal Signaling
Target	iGluR; iGluR
Biological Activity	GYKI53655 hydrochloride is an alpha-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA) antagonist. IC50 & Target: AMPA^{[1] In Vitro: GYKI53655 hydrochloride (LY300168) inhibits alpha-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA) (10 uM)-induced responses with IC₅₀ value of 5.9+/-0.1 uM. GYKI53655 hydrochloride inhibits AMPA (10 uM) responses in recombinant G1uR4 expressing HEK293 cells with IC₅₀ value of 4.6+/-0.4 uM. Using 3 uM cyclothiazide the inhibition produced by GYKI53655 hydrochloride is 79+/-2% (n=4 cells). GYKI53655 hydrochloride produces only small inhibitions of kainate-induced currents at 30 uM and inhibits kainate-induced currents at a concentration of 100 uM by 12+/-2 (n=4) and 18+/-4 (n=4), respectively. GYKI53655 hydrochloride inhibits AMPA receptor-mediated responses in cerebella Purkinje neurons with an IC₅₀ value of 1.5+/-0.1 uM^[1]. In Vivo: GYKI53655 hydrochloride (4 mg/kg) is found to have a short-lasting depressant effect on neuronal responses to iontophoretic alpha-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA), with a half-recovery time of approximately 7 min. GYKI53655 hydrochloride (4 and 8 mg/kg) substantially depresses or completely abolishes AMPA responses. Results demonstrate the dose-dependence of GYKI53655 hydrochloride (2 to 8 mg/kg) in depressing responses to AMPA. At the highest doses tested, GYKI53655 hydrochloride reduces AMPA responses to a comparable degree^[2]. Tonic fit and death are completely prevented by GYKI53655 hydrochloride at dose over 5.0 mg/kg. The ED₅₀ value of GYKI53655 hydrochloride is 2.2 mg/kg i.p. The maximal effects of GYKI53655 hydrochloride lasts 3 h then the exit inhibition effect of GYKI53655 hydrochloride falls to 20% 1 h later^[3].}

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Amount: 5mg

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