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Documentos Principais

SML3013

Sigma-Aldrich

LY2886721

≥98% (HPLC)

Sinônimo(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

Fórmula empírica (Notação de Hill):
C18H16F2N4O2S
Número CAS:
Peso molecular:
390.41
Número MDL:
Código UNSPSC:
12352200
NACRES:
NA.77

Nível de qualidade

Ensaio

≥98% (HPLC)

Formulário

powder

cor

white to beige

solubilidade

DMSO: 2 mg/mL, clear

temperatura de armazenamento

2-8°C

cadeia de caracteres 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

chave InChI

NIDRNVHMMDAAIK-YPMLDQLKSA-N

Ações bioquímicas/fisiológicas

Orally active, potent and selective β-secretase (BACE) active site inhibitor with amyloid β-lowering efficacy in cultures and in animal models in vivo.
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.).

Código de classe de armazenamento

11 - Combustible Solids

Classe de risco de água (WGK)

WGK 3

Ponto de fulgor (°F)

Not applicable

Ponto de fulgor (°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
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
Claire S Durrant et al.
Cell death & disease, 11(2), 98-98 (2020-02-08)
Amyloid beta peptides (Aβ) proteins play a key role in vascular pathology in Alzheimer's Disease (AD) including impairment of the blood-brain barrier and aberrant angiogenesis. Although previous work has demonstrated a pro-angiogenic role of Aβ, the exact mechanisms by which
Allison Knupp et al.
Cell reports, 31(9), 107719-107719 (2020-06-04)
SORL1/SORLA is a sorting receptor involved in retromer-related endosomal traffic and an Alzheimer's disease (AD) risk gene. Using CRISPR-Cas9, we deplete SORL1 in hiPSCs to ask if loss of SORL1 contributes to AD pathogenesis by endosome dysfunction. SORL1-deficient hiPSC neurons

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