A positive allosteric modulator of GABAA receptors; potentiates GABA-induced currents in LTK cells expressing α4β2γ2 subunit-containing GABAA receptors and CHO cells expressing α4β3δ subunit-containing GABAA receptors (EC50s = 375 and 299 nM

SAGE-217 – 1 mg

Brand:
Cayman
CAS:
1632051-40-1
Storage:
-20
UN-No:
Non-Hazardous - /

SAGE-217 is a positive allosteric modulator of GABAA receptors.{59529} It potentiates GABA-induced currents in LTK cells expressing α4β2γ2 subunit-containing GABAA receptors and CHO cells expressing α4β3δ subunit-containing GABAA receptors (EC50s = 375 and 299 nM, respectively). SAGE-217 (0.3-10 mg/kg, i.p.) reduces the number of seizures induced by pentylenetetrazole (PTZ; Item No. 18682) in mice. It also inhibits electrographic and behavioral seizure activity in a rat model of lithium-pilocarpine induced status epilepticus.  

 

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SKU: 31755 - 1 mg Category:

Description

A positive allosteric modulator of GABAA receptors; potentiates GABA-induced currents in LTK cells expressing α4β2γ2 subunit-containing GABAA receptors and CHO cells expressing α4β3δ subunit-containing GABAA receptors (EC50s = 375 and 299 nM, respectively); reduces the number of PTZ-induced seizures in mice from 0.3-10 mg/kg, i.p.

Formal name: 1-[(3α,5β)-3-hydroxy-3-methyl-20-oxo-19-norpregnan-21-yl]-1H-pyrazole-4-carbonitrile

Synonyms:  S-812217|SGE 797

Molecular weight: 409.6

CAS: 1632051-40-1

Purity: ≥98%

Formulation: A crystalline solid

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