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Zuranolone

Chemical Structure : Zuranolone

CAS No.: 1632051-40-1

Zuranolone (SAGE-217, SAGE217)

Catalog No.: PC-38319Not For Human Use, Lab Use Only.

Zuranolone (SAGE-217) is an orally active, positive allosteric modulator of the GABAA receptor with EC50 of 375/299 nM (α1β2γ2/α4β3δ).

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Biological Activity

Zuranolone (SAGE-217) is an orally active, positive allosteric modulator of the GABAA receptor with EC50 of 375/299 nM (α1β2γ2/α4β3δ).
Zuranolone (SAGE-217)shows an IC50 of 7 nM in in the [35S]TBPS binding assays.
Zuranolone (SAGE-217) displays remarkably selectivity against a broad panel of enzymes and receptors (78 targets) in a pan-screen.
Acute administration of SAGE-217 (0.3-10 mg/kg, ip) effectively reduced pentylenetretazol (PTZ)-induced seizures in mice, as well as producing a dose-dependent anticonvulsant effect in the mouse 6 Hz electrical stimulation model.

Physicochemical Properties

M.Wt 409.6
Formula C25H35N3O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 1 Month
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

3α-Hydroxy-3β-methyl-21-(4-cyano-1H-pyrazol-1′-yl)-19-nor-5β-pregnan-20-one

References

1. Martinez Botella G, et al. J Med Chem. 2017 Sep 28;60(18):7810-7819.

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