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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-GABA Receptor-Zuranolone
Zuranolone

Chemical Structure : Zuranolone

CAS No.: 1632051-40-1

Zuranolone (SAGE-217, SAGE217)

货号: 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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10 mg ¥1380 In stock
25 mg ¥2180 In stock
50 mg ¥3580 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 409.6
分子式 C25H35N3O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -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

参考文献

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

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