Atabecestat (C09-1102-097)

Atabecestat (JNJ-54861911) is a potent brain-penetrant and orally active β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor, achieves robust and high CSF Aβ reduction. Atabecestat s tolerated and displays a sustained pharmacokinetic (PK) and pharmacodynamic (PD) characteristics. Atabecestat has the potential for Alzheimer's Disease treatmentIn VivoAtabecestat (100 and 300 mg/kg; p.o. once daily for 3 days) reduces the human Aβ levels in mice. Atabecestat (300 mg/kg; p.o. once) inhibits the exacerbation of vascular abnormalities in APPPS1 mice with 3D6 treatment. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: 5-week-old APPPS1 miceDosage: 100 and 300 mg/kg Administration: Oral gavage; 100 and 300 mg/kg; once daily for 3 days Result: Reduced the level of human Aβ 1-40 and Aβ 1-42 levels in the brain of APPPS1 mice at a dose of 300 mg/kg and resulted in less reduction of human Aβ levels at 24 h with a dose of 100 mg/kg.Form:SolidIC50& Target:BACE1. Specification: 0.98 Molecular Formula: C18H14FN5OS Molecular Weight: 367.4 EC Number: 807-396-1 PubChem CID: 68254185 Isomeric SMILES: C[C@]1(C=CSC(=N1)N)C2=C(C=CC(=C2)NC(=O)C3=NC=C(C=C3)C#N)F