GYKI-47261 (dihydrochloride)

GYKI-47261 dihydrochloride is a competitive, orally active, and selective AMPA receptor antagonist with an IC50 of 2.5 μM. GYKI-47261 has broad spectrum anticonvulsive activity and neuroprotective effects. GYKI-47261 dihydrochloride is also a potent inducer of CYP2E1[1][2].

Product Specifications

CAS Number

[1217049-32-5]

UNSPSC

12352005

Target

Cytochrome P450; iGluR

Type

Reference compound

Related Pathways

Membrane Transporter/Ion Channel; Metabolic Enzyme/Protease; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/gyki-47261-dihydrochloride.html

Solubility

10 mM in DMSO

Smiles

NC1=CC=C(C2=NN3C(CC4=CC=C(Cl)C=C42)=NC(C)=C3)C=C1.[H]Cl.[H]Cl

Molecular Formula

C18H17Cl3N4

Molecular Weight

395.71

References & Citations

[1]Abrahám G, et al. New non competitive AMPA antagonists. Bioorg Med Chem. 2000;8 (8) :2127-2143.|[2]Tamási V, et al. GYKI-47261, a new AMPA [2-amino-3- (3-hydroxymethylisoxazole-4-yl) propionic acid] antagonist, is a CYP2E1 inducer. Drug Metab Dispos. 2003;31 (11) :1310-1314.