LY2886721 (Synonyms: β-Secretase) |
| Catalog No.GC17227 |
LY2886721 es un inhibidor potente, selectivo y oralmente activo de la proteÍna precursora de amiloide del sitio beta que escinde la enzima 1 (BACE1) con una IC50 de 20,3 nM para BACE1 humana recombinante.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1262036-50-9
Sample solution is provided at 25 µL, 10mM.
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LY2886721 is an oral and furothiazine-based inhibitor of β site-amyloid protein cleaving enzyme (BACE) with IC50 of 20.3nM. This product has the potency for the treatment of Alzheimer's disease.
BACE, also known as Beta-Secretase 1, is an aspartic-acid protease that plays important role in the formation of myelin sheaths in peripheral nerve cells.
In vitro, treatment of LY2886721 leads to the inhibition of Aβ in HEK293Swe with IC50 of 18.7nM and PDAPP neuronal culture with IC50 10.7 nM1. LY2886721 decreases CSF sAPPβ and increases CSF sAPPα in a dose- dependent manner 2.
In PDAPP mice, oral administration of LY2886721 resulted in a reduction in brain Aβ, C99 and sAPPβ in a dose-dependent pattern 2. Aβ levels in the brain were decreased by 20% -65% as compared with the vehicle-treated groups 3 hours after treatment of LY2886721 at a dosage of 3-30 mg/kg per mice. In addition, LY2886721 significantly lowers plasma and CSF Aβs in the MAD study 1.
References:
1. Vassar R. BACE1 inhibitor drugs in clinical trials for Alzheimer's disease. Alzheimer's research & therapy. 2014;6(9):89.
2. Nishitomi K, Sakaguchi G, Horikoshi Y, et al. BACE1 inhibition reduces endogenous Abeta and alters APP processing in wild-type mice. Journal of neurochemistry. 2006;99(6):1555-1563.
Average Rating: 5 (Based on Reviews and 24 reference(s) in Google Scholar.)
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