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安全信息

S4562

Sigma-Aldrich

β-Secretase inhibitor

≥97% (HPLC), powder

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About This Item

经验公式（希尔记法）:
C73H118N16O27
分子量:
1651.81
MDL编号:
MFCD02683580
UNSPSC代码:
12352200
NACRES:
NA.77

生物来源

synthetic (organic)

质量水平

200

方案

≥97% (HPLC)

表单

powder

分子量

~_1.65 kDa

颜色

white

mp

200 °C

溶解性

DMSO: soluble

运输

dry ice

储存温度

−20°C

SMILES字符串

N([C@H]([C@@H](O)CC(=O)N[C@@H](C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)O)CC(C)C)C(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](N)CCCCN)[C@H](O)C)CCC(=O)O)C

InChI

1S/C73H118N16O27/c1-11-37(8)59(88-66(108)45(23-27-56(101)102)79-63(105)43(21-25-54(97)98)81-72(114)60(39(10)91)89-62(104)41(75)19-15-16-28-74)71(113)85-49(33-90)68(110)80-44(22-26-55(99)100)65(107)87-58(36(6)7)70(112)83-47(31-51(76)93)67(109)82-46(29-34(2

InChI key

CQTBDEGWLSDJEP-JMAXQNTPSA-N

Amino Acid Sequence

Lys-Thr-Glu-Glu-Ile-Ser-Glu-Val-Asn-Sta-Val-Ala-Glu-Phe

一般描述

β-Site amyloid precursor protein (APP) cleaving enzyme-1 (BACE1), an aspartic protease belongs to the protease family of enzymes comprises of six luminal cysteine residues. These residues help in the formation of three intermolecular disulfide bonds and N-linked glycosylation sites.

应用

β-Secretase inhibitor has been used as β-site amyloid precursor protein (APP) cleaving enzyme-1 (BACE1) inhibitor in BACE1 inhibitor assay.(2)
β-Secretase inhibitor may be used to inhibit BACE1 in studies related to AD.

生化/生理作用

β-Site amyloid precursor protein (APP) cleaving enzyme-1 (BACE1) is a β-secretase that initiates the production of amyloid protein in Alzheimer′s dieases (AD) patients. β-Secretase inhibitors decrease the generation of β amyloid and formation of amyloid plaques typical of AD.

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

个人防护装备

Eyeshields, Gloves, type N95 (US)

法规信息

新产品

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分析证书(COA)

Lot/Batch Number
SLBZ0604
SLBX6274
SLBT2813
SLBP1431V
SLBM3424V

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B J Baranowski et al.
Physiological reports, 12(16), e70001-e70001 (2024-08-20)
Brain-derived neurotrophic factor (BDNF) content and signaling has been identified as one potential regulator of amyloid precursor protein (APP) processing. Recently published work has demonstrated that BDNF reduces BACE1 activity while also elevating the inhibition of GSK3β in the prefrontal
Jungmi Lee et al.
Analytica chimica acta, 1022, 89-95 (2018-05-08)
Amyloid-β (Aβ) is generated by proteolytic processing of amyloid precursor protein (APP) by beta-secretase (BACE-1) and gamma-secretase. Amyloid-β is responsible for the formation of senile plaques in Alzheimer's disease (AD). Consequently, inhibition of β-secretase (BACE-1), a rate-limiting enzyme in the
beta-secretase inhibitor; a promising novel therapeutic drug in Alzheimer?s disease
Menting KW, et al.
Frontiers in Aging Neuroscience, 6, 165-165 (2014)
S Sinha et al.
Nature, 402(6761), 537-540 (1999-12-11)
Proteolytic processing of the amyloid precursor protein (APP) generates amyloid beta (Abeta) peptide, which is thought to be causal for the pathology and subsequent cognitive decline in Alzheimer's disease. Cleavage by beta-secretase at the amino terminus of the Abeta peptide
Hans Hilpert et al.
Journal of medicinal chemistry, 56(10), 3980-3995 (2013-04-18)
An extensive fluorine scan of 1,3-oxazines revealed the power of fluorine(s) to lower the pKa and thereby dramatically change the pharmacological profile of this class of BACE1 inhibitors. The CF3 substituted oxazine 89, a potent and highly brain penetrant BACE1
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