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SML3013

Sigma-Aldrich

LY2886721

≥98% (HPLC)

Synonym(e):

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

Empirische Formel (Hill-System):
C18H16F2N4O2S
CAS-Nummer:
1262036-50-9
Molekulargewicht:
390.41
MDL-Nummer:
MFCD22124078
UNSPSC-Code:
12352200
NACRES:
NA.77

Qualitätsniveau

100

Assay

≥98% (HPLC)

Form

powder

Farbe

white to beige

Löslichkeit

DMSO: 2 mg/mL, clear

Lagertemp.

2-8°C

SMILES String

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

InChIKey

NIDRNVHMMDAAIK-YPMLDQLKSA-N

Biochem./physiol. Wirkung

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.).

Lagerklassenschlüssel

11 - Combustible Solids

WGK

WGK 3

Flammpunkt (°F)

Not applicable

Flammpunkt (°C)

Not applicable

Analysenzertifikate (COA)

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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
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
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
Doaa M Hanafy et al.
Nutrients, 12(5) (2020-05-14)
Alzheimer's disease (AD) is a progressive neurodegenerative disorder with an unclear cause. It appears that multiple factors participate in the process of neuronal damage including oxidative stress and accumulation of the protein amyloid β (Aβ) in the brain. The search
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
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