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)
- color
- White to off-white
- InChI
- InChI=1S/C18H16F2N4O2S/c19-11-1-4-15(22-6-11)16(25)23-12-2-3-14(20)13(5-12)18-9-26-7-10(18)8-27-17(21)24-18/h1-6,10H,7-9H2,(H2,21,24)(H,23,25)/t10-,18-/m0/s1
- InChIKey
- NIDRNVHMMDAAIK-YPMLDQLKSA-N
- SMILES
- C1(C(NC2=CC=C(F)C([C@]34COC[C@@]3([H])CSC(N)=N4)=C2)=O)=NC=C(F)C=C1
LY2886721 Usage And Synthesis
Uses
LY2886721 is a BACE inhibitor used to treat Alzheimer's disease.
Uses
LY2886721 is a potent, selective and orally active beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor with an IC50 of 20.3 nM for recombinant human BACE1. LY2886721 is selectivity against cathepsin D, pepsin, and renin, but lacking selectivity against BACE2 (IC50 of 10.2 nM). LY2886721 can across blood-brain barrier and has the potential for Alzheimer's disease treatment[1].
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.
in vivo
LY2886721 (3-30 mg/kg; oral administration; PDAPP mice) treatment significantly reduces the hippocampal and cortical levels of Aβ1-x. LY2886721 treatment results in significant reduction of brain parenchymal levels of C99 and sAPPβ[1].
| Animal Model: | Female hemizygous APPV717F transgenic mice (PDAPP) (2-3 months old)[1] |
| Dosage: | 3 mg/kg, 10 mg/kg, 30 mg/kg |
| Administration: | Oral administration |
| Result: | Hippocampal and cortical levels of Aβ1-x were significantly reduced. |
target
BACE
IC 50
BACE1
References
1. vassar r. bace1 inhibitor drugs in
LY2886721Supplier
- Tel
- sales@boylechem.com
- Tel
- +86-21-20908456
- sales@BioChemBest.com
- Tel
- 0571-82693216
- info@yuhaochemical.com
- Tel
- 0411-62910999 13889544652
- sales@meilune.com
- Tel
- 4000-027-021 |24 +86-13986109188 | +86-15623472865 | +81-08033611988