| CAS | 314266-76-7 |
| Sequence | H-Glu-Val-Asn-[(2R,4S,5S)-5-amino-4-hydroxy-2,7-dimethyl-octanoyl]-Ala-Glu-Phe-OH |
| Sequence Single | EVN[(2R,4S,5S)-5-amino-4-hydroxy-2,7-dimethyl-octanoyl]AEF |
| Molecular Formula | C41H64N8O14 |
| Molecular Weight | 893.01 |
| Technology | Synthetic |
| Storage | -20°C, avoid light, cool and dry place |
| Application | Alzheimer’s Disease |
| Description | OM99-2, an eight residue peptidomimetic, tight-binding inhibitor of human brain memapsin-2 (β-secretase) with a Ki value of 9.58 nM. OM99-2 is significantly advanced the development of BACE1 inhibitor. OM99-2 has the potential for the research of the Alzheimer’s disease. |
| References | 1. Quantification of cathepsins B and L in cells. R.Xing et al., Biochem. J., 332, 499 (1998) 2. Design of Potent Inhibitors for Human Brain Memapsin 2 (β-Secretase). Ghosh AK, et al. J Am Chem Soc. 2000;122(14):3522-3523. 3. Targeting Amyloidogenic Processing of APP in Alzheimer’s Disease. Zhao J, et al. Front Mol Neurosci. 2020;13:137. Published 2020 Aug 4. 4. Aspartic peptidase inhibitors: implications in drug development. Dash C, et al. Crit Rev Biochem Mol Biol. 2003;38(2):89-119. 5. Determination of the active site protonation state of beta-secretase from molecular dynamics simulation and docking experiment: implications for structure-based inhibitor design. Park H, et al. J Am Chem Soc. 2003;125(52):16416-16422. |