Aβ42-IN-1, compound 1v, is a novel, potent and orally active γ-secretase modulator (GSM). Aβ42-IN-1 potently reduced Aβ42 levels with an IC 50 value of 0.091 μM in cultured cells without inhibiting CYP3A4. Aβ42-IN-1 shows a sustained pharmacokinetic profile.

γ-secretase modulator:0.091 µM

Aβ42-IN-1 (orally adminstation; 30 mg/kg) demonstrates a good pharmacokinetic profile in mice, significantly reduces Aβ42 levels in the brain and plasma, by 36% and 66%, respectively. while the brain/plasma ratio of 1v is slightly lower than that of 1a [1]. Animal Model: 8- week-old male ddY mice Dosage: 30 mg/kg Administration: Orally adminstation; 30 mg/kg Result: Reduced Aβ42 levels in the brain and plasma, by 36% and 66%, respectively.