| Bioactivity | 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 IC50 value of 0.091 µM without CYP3A4 inhibition. Aβ42-IN-1 shows a sustained pharmacokinetic profile. |
| Target | IC50: 0.091 µM (γ-secretase modulator) |
| In Vivo | Aβ42-IN-1 (orally adminstation; 30 mg/kg)shows 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: |
| Name | Aβ42-IN-1 |
| Formula | C29H27ClN4O2 |
| Molar Mass | 499.00 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Sekioka R, et al. Discovery of N-ethylpyridine-2-carboxamide derivatives as a novel scaffold for orally active γ-secretase modulators.Bioorg Med Chem. 2019 Nov 6:115132. |