LY2886721 - CAS 1262036-50-9
Catalog number:
1262036-50-9
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C18H16F2N4O2S
Molecular Weight:
390.41
COA:
Inquire
Targets:
β-secretase
Description:
LY2886721, under the IUPAC name N-(3-(2-amino-4a,5,7,7a-tetrahydro-4H-furo(3,4-d)(1,3)thiazin-7a-yl)-4-fluorophenyl)-5-fluoropicolinamide, is the first oral small molecule inhibitting Beta secretase (BACE) to reach Phase 2 clinical research. It was developed by Eli Lilly & Co. with the potention to treat Alzheimer's Disease.
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Brife Description:
The first oral small molecule inhibit Beta secretase (BACE) to reach Phase 2 clinical research.
Related CAS:
262036-49-6 (HCl )
Appearance:
Solid powder
Synonyms:
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; LY 2886721
Solubility:
Soluble to 28mg/mL in DMSO
Storage:
Store in a cool and dry place and at 0 - 4℃ for short term (days to weeks) or -44℃ for long term (months to years).
MSDS:
Inquire
InChIKey:
NIDRNVHMMDAAIK-YPMLDQLKSA-N
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
Canonical SMILES:
O=C(NC1=CC=C(F)C([C@@]23N=C(N)SC[C@]2([H])COC3)=C1)C4=NC=C(F)C=C4
1.The potent BACE1 inhibitor LY2886721 elicits robust central Aβ pharmacodynamic responses in mice, dogs, and humans.
May PC1, Willis BA1, Lowe SL2, Dean RA1, Monk SA1, Cocke PJ1, Audia JE1, Boggs LN1, Borders AR1, Brier RA1, Calligaro DO1, Day TA1, Ereshefsky L3, Erickson JA1, Gevorkyan H4, Gonzales CR1, James DE1, Jhee SS3, Komjathy SF1, Li L1, Lindstrom TD1, Mathes BM J Neurosci. 2015 Jan 21;35(3):1199-210. doi: 10.1523/JNEUROSCI.4129-14.2015.
BACE1 is a key protease controlling the formation of amyloid β, a peptide hypothesized to play a significant role in the pathogenesis of Alzheimer's disease (AD). Therefore, the development of potent and selective inhibitors of BACE1 has been a focus of many drug discovery efforts in academia and industry. Herein, we report the nonclinical and early clinical development of LY2886721, a BACE1 active site inhibitor that reached phase 2 clinical trials in AD. LY2886721 has high selectivity against key off-target proteases, which efficiently translates in vitro activity into robust in vivo amyloid β lowering in nonclinical animal models. Similar potent and persistent amyloid β lowering was observed in plasma and lumbar CSF when single and multiple doses of LY2886721 were administered to healthy human subjects. Collectively, these data add support for BACE1 inhibition as an effective means of amyloid lowering and as an attractive target for potential disease modification therapy in AD.
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CAS 1262036-50-9 LY2886721

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