Potent and selective β-secretase (BACE) inhibitor (IC50 values are 10.2 and 20.3 nM for humanBACE2 and BACE1, respectively). Displays >5,000-fold selectivity for BACE over other proteases including cathepsin D, pepsin and renin. Inhibits Aβ1-40 and Aβ1-42 production in cells expressing mutated APP. Reduces hippocampal and cortical Aβ and sAPPβ levels in an Alzheimer's disease mouse model.
OM99-2 TFA is an eight-residue peptidomimetic compound, functioning as a tight-binding inhibitor of human brain memapsin 2. It exhibits a high affinity for the target with a Ki value of 9.58 nM, making it a promising candidate in the development of BACE1 inhibitors. Due to its potential, OM99-2 presents opportunities for further research in the field of Alzheimer's disease.
OM99-2 is an eight-residue peptidomimetic with a high affinity for human brain memapsin 2, exhibiting a Ki value of 9.58 nM. This compound represents a significant advancement in the development of BACE1 inhibitors and holds potential for the study of Alzheimer's disease.