| Bioactivity | GYKI-47261 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 is also a potent inducer of CYP2E1[1][2]. |
| In Vivo | GYKI-47261 (6 mg/kg; i.v.) shows antiischemice effect in a transient focal ischemia model, in rats. GYKI-47261 (p.o.) potently mitigated the tremor induced by oxotremorine with ED50 of 16.8 mg/kg in male CD1 mice[1].GYKI-47261(20 mg/kg; i.p.) reverses the dopamine depleting effect of MPTP[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: |
| CAS | 220445-20-5 |
| Formula | C18H15ClN4 |
| Molar Mass | 322.79 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. |
GYKI-47261
CAS: 220445-20-5 F: C18H15ClN4 W: 322.79
GYKI-47261is a competitive, orally active, and selective AMPA receptor antagonist with an IC50 of 2.5 μM. GYKI-47261 ha
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