LY2886721
LY2886721 Basic information
- Product Name:
- LY2886721
- Synonyms:
-
- LY2886721
- N-[3-[(4aS,7aS)-2-Amino-4a,5-dihydro-4H-furo[3,4-d][1,3]thiazin-7a(7H)-yl]-4-fluorophenyl]-5-fluoro-2-pyridinecarboxamide
- LY2886721 HCL SALT
- LY2886721HCL
- N-[3-[(4aS,7aS)-2-Amino-4a,5-dihydro-4H-furo[3,4-d][1,3]thiazin-7a(7H)-yl]-4-fluorophenyl]-5-fluoro-2-pyridinecarboxamide LY2886721
- LY2886721, >=98%
- 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
- LY2886721/LY-2886721
- CAS:
- 1262036-50-9
- MF:
- C18H16F2N4O2S
- MW:
- 390.41
- Product Categories:
-
- Inhibitors
- Mol File:
- 1262036-50-9.mol
LY2886721 Chemical Properties
- Density
- 1.57
- storage temp.
- Store at -20°C
- solubility
- insoluble in H2O; insoluble in EtOH; ≥19.52 mg/mL in DMSO
- form
- solid
- pka
- 10.08±0.70(Predicted)
LY2886721 Usage And Synthesis
Uses
LY2886721 is a BACE inhibitor used to treat Alzheimer's disease.
Biological Activity
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 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.
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.
target
BACE
References
1. vassar r. bace1 inhibitor drugs in
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