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SML3013

Sigma-Aldrich

LY2886721

≥98% (HPLC)

Synonyme(s) :

LY 2886721, LY-2886721, 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, 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

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About This Item

Formule empirique (notation de Hill):
C18H16F2N4O2S
Numéro CAS:
1262036-50-9
Poids moléculaire :
390.41
Numéro MDL:
MFCD22124078
Code UNSPSC :
12352200
Nomenclature NACRES :
NA.77

Niveau de qualité

100

Pureté

≥98% (HPLC)

Forme

powder

Couleur

white to beige

Solubilité

DMSO: 2 mg/mL, clear

Température de stockage

2-8°C

Chaîne SMILES 

FC1=CC=C(NC(C2=CC=C(C=N2)F)=O)C=C1[C@@]34[C@@](CSC(N)=N4)([H])COC3

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

Clé InChI

NIDRNVHMMDAAIK-YPMLDQLKSA-N

Actions biochimiques/physiologiques

Y2886721 is an orally active, potent and selective β-secretase (BACE) active site inhibitor (human BACE1/2 IC50 = 20.3/10.2 nM; cathepsin D/pepsin/renin IC50 >10 μM). Y2886721 exhibits amyloid β-lowering efficacy in cultures (Aβ1-40/Aβ1-42 IC50 = 18.5/19.7 nM with APP751 Swedish mutation-expressing HEK293 and 10.7/9.2 nM with primary cortical neurons from PDAPP transgenic mouse embryos) and in animal models in vivo (3-30 mg/kg PDAPP mice, 1.5 mg/kg beagle dogs; p.o.).

Code de la classe de stockage

11 - Combustible Solids

Classe de danger pour l'eau (WGK)

WGK 3

Point d'éclair (°F)

Not applicable

Point d'éclair (°C)

Not applicable

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Tugce Munise Satir et al.
Alzheimer's research & therapy, 12(1), 63-63 (2020-05-28)
Alzheimer's disease (AD) is the most common form of age-related neurodegenerative diseases. Cerebral deposition of Aβ peptides, especially Aβ42, is considered the major neuropathological hallmark of AD and the putative cause of AD-related neurotoxicity. Aβ peptides are produced by sequential
Patrick C May et al.
The Journal of neuroscience : the official journal of the Society for Neuroscience, 35(3), 1199-1210 (2015-01-23)
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
Jan Schejbal et al.
Journal of separation science, 42(5), 1067-1076 (2019-01-22)
Capillary electrophoresis integrated immobilized enzyme reactors are becoming an increasingly popular alternative for enzyme kinetic and inhibition assays thanks to their unique set of features including cost effectiveness, repeated use of the enzyme, minuscule sample consumption, rapid analysis time and
Ling Li et al.
Cell proliferation, 53(4), e12798-e12798 (2020-03-28)
Alzheimer's disease (AD) is the most common neurodegenerative disease which is characterized by the formation of amyloid beta (Aβ) plaques and neurofibrillary tangles. These abnormal proteins induce disturbance in mitochondrial dynamics and defect in autophagy system. Since presenilin-1 (PS1) is
Akihiro Takano et al.
Journal of nuclear medicine : official publication, Society of Nuclear Medicine, 60(7), 992-997 (2018-12-12)
β-secretase 1 (BACE1) is a key enzyme in the generation of β-amyloid, which is accumulated in the brain of Alzheimer disease patients. PF-06684511 was identified as a candidate PET ligand for imaging BACE1 in the brain and showed high specific
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