LY2886721, BACE-1 inhibitor (ab223886)
- Datasheet
- References
Overview
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Product name
LY2886721, BACE-1 inhibitor -
Description
Potent and selective BACE-1 inhibitor -
Alternative names
- LY2886721
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Biological description
Potent and selective BACE-1 inhibitor (IC50 = 20.3 nM for recombinant hBACE-1). Human BACE2 is inhibited with an IC50 of 10.2 nM. Does not inhibit other aspartyl proteases such as cathepsin D, pepsin, and renin. A potential agent to treat Alzheimer’s Disease. Inhibits production of Aβ in HEK-293 Swe cells (IC50 values are 18.5 nM and 19.7 nM for Aβ1-40 and Aβ1-42 respectively) and in PDAPP neuronal cells (IC50 ~10 nM). Reduces dose-dependently brain levels of Aβ, C99 and sAPPβ in orally administered mouse model and plasma Aβ in dog model. Ppenetrates the blood-brain barrier.
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Purity
> 98% -
CAS Number
1262036-50-9 -
Chemical structure
Properties
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Chemical name
N-(3-((4aS,7aS)-2-Amino-4a,5,7,7a-tetrahydro-4H-furo[3,4-d][1,3]thiazin-7a-yl)-4-fluorophenyl)-5-fluoropicolinamide
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Molecular weight
390.41 -
Molecular formula
C18H16F2N4O2S -
PubChem identifier
49837968 -
Storage instructions
Shipped at 4°C. Store at -20°C. Store In the Dark. Store under desiccating conditions. -
Solubility overview
Soluble in DMSO to 20 mM, in Ethanol < 2 mM
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SMILES
C1[C@H]2CSC(=N[C@]2(CO1)C3=C(C=CC(=C3)NC(=O)C4=NC=C(C=C4)F)F)N -
Source
Synthetic
References
This product has been referenced in:
- May PC et al. The potent BACE1 inhibitor LY2886721 elicits robust central Aß pharmacodynamic responses in mice, dogs, and humans. J Neurosci 35:1199-210 (2015). Read more (PubMed: 25609634) »
- Qi Y et al. Longitudinal testing of hippocampal plasticity reveals the onset and maintenance of endogenous human Aß-induced synaptic dysfunction in individual freely behaving pre-plaque transgenic rats: rapid reversal by anti-Aß agents. Acta Neuropathol Commun 2:175 (2014). Read more (PubMed: 25540024) »
- Lahiri DK et al. Lessons from a BACE1 inhibitor trial: off-site but not off base. Alzheimers Dement 10:S411-9 (2014). Read more (PubMed: 24530026) »
