SAGE-217

SAGE-217 is a positive allosteric modulator of GABAA receptors. It potentiates GABA-induced currents in LTK cells expressing alpha4beta2gamma2 subunit-containing GABAA receptors and CHO cells expressing alpha4beta3delta 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, Cay-18682) in mice. It also inhibits electrographic and behavioral seizure activity in a rat model of lithium-pilocarpine induced status epilepticus.Formal Name: 1-[(3alpha,5beta)-3-hydroxy-3-methyl-20-oxo-19-norpregnan-21-yl]-1H-pyrazole-4-carbonitrile. CAS Number: 1632051-40-1. Synonyms: S-812217, SGE 797, Zuranolone. Molecular Formula: C25H35N3O2. Formula Weight: 409.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMF:PBS (pH 7.2) (1:2): 0.33 mg/ml, DMSO: 10 mg/ml. lambdamax: 215 nm. SMILES: C[C@@]12[C@](CC[C@@H]2C(CN3C=C(C=N3)C#N)=O)([H])[C@@]4([H])[C@@](CC1)([H])[C@]5([H])[C@](C[C@](O)(CC5)C)([H])CC4. InChi Code: InChI=1S/C25H35N3O2/c1-24(30)9-7-18-17(11-24)3-4-20-19(18)8-10-25(2)21(20)5-6-22(25)23(29)15-28-14-16(12-26)13-27-28/h13-14,17-22,30H,3-11,15H2,1-2H3/t17-,18+,19-,20-,21+,22-,24-,25+/m1/s1. InChi Key: HARRKNSQXBRBGZ-GVKWWOCJSA-N.