GABAA receptor modular-3 

GABAA receptor modular-3 (Compound S28) is a modulator for (γ-aminobutyric acid)A receptor (GABAA receptor), with EC₅₀ of 56 nM and 10 nM, for α1β2γ2 and α4β3δ subtype. GABAA receptor modular-3 exhibits good pharmacokinetic characteristics in rats. GABAA receptor modular-3 is slightly toxic toxicity in rats with a loss of rollover reflex (LORR) threshold dose of 23.3 μmol/kg, and exhibits potential ameliorating the postpartum depression^[1].

EC₅₀: 56 nM (GABAA receptor α1β2γ2); 10 nM (GABAA receptor α4β3δ)

514.61

C₂₈H₃₆F₂N₄O₃

3021554-08-2

C[C@@]12[C@](CC[C@@H]2C(CN3C=NN(C4=CC(F)=NC(F)=C4)C3=O)=O)([H])[C@]5([H])CC[C@]6([H])C[C@@](O)(C)CC[C@]6([H])[C@@]5([H])CC1

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Ma M, et al., Synthesis and evaluation of neuroactive steroids with novel pharmacophore at C-21 let identify a compound with advantageous PK profile and higher EC50 and Emax as PAM on GABAA receptor. Eur J Med Chem. 2024 Jun 22;276:116602.  [Content Brief]