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Merck
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Key Documents

SML3144

Sigma-Aldrich

delta-Secretase inhibitor, CP11

≥95% (HPLC)

同義詞:

δ-Secretase inhibitor 11, δ-Secretase inhibitor, compound 11, δ-Secretase inhibitor, compound 11A, 7-(4-Morpholinyl)-2,1,3-benzoxadiazol-4-amine, 7-(Morpholin-4-yl)-2,1,3-benzoxadiazol-4-amine, 7-Morpholin-4-yl-benzo[1,2,5]oxadiazol-4-ylamine, CP11, CPA, delta-Secretase inhibitor, compound 11

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About This Item

經驗公式(希爾表示法):
C10H12N4O2
CAS號碼:
分子量::
220.23
MDL號碼:
分類程式碼代碼:
12352200
NACRES:
NA.28

品質等級

化驗

≥95% (HPLC)

形狀

powder

顏色

, Faint Brown to dark red

溶解度

DMSO: 2 mg/mL, clear

儲存溫度

2-8°C

生化/生理作用

Compound 11 (CP11) is an orally active and brain-penetrant delta-secretase (δ-secretase; AEP) inhibitor that selectively blocks AEP (IC50 = 710 nM) but not other related cysteine proteases (Caspase-3/-8 IC50 = 31.86/86.71 μM, Cathepsin-S/-L IC50 >200 μM) via a dual active site-directed and allosteric mode of inhibition. CP11 inhibits Pala cellular AEP activity in cultures (IC50 = 800 nM) and improves cognitive functions in murine models of Alzheimer′s disease (AD) in vivo (10 mg/kg tau P301S or 5xFAD mice via daily p.o.) by reducing tau and APP cleavage, ameliorating synapse loss and augmenting long-term potentiation.

象形圖

Skull and crossbones

訊號詞

Danger

危險聲明

危險分類

Acute Tox. 3 Dermal - Acute Tox. 4 Oral

儲存類別代碼

6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable


分析證明 (COA)

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Ju Wang et al.
Translational neurodegeneration, 10(1), 12-12 (2021-04-02)
Currently, there is no cure for Alzheimer's disease (AD). Therapeutics that can modify the early stage of AD are urgently needed. Recent studies have shown that the pathogenesis of AD is closely regulated by an endo/lysosomal asparaginyl endopeptidase (AEP). Inhibition
Zhentao Zhang et al.
Nature communications, 8, 14740-14740 (2017-03-28)
δ-secretase, also known as asparagine endopeptidase (AEP) or legumain, is a lysosomal cysteine protease that cleaves both amyloid precursor protein (APP) and tau, mediating the amyloid-β and tau pathology in Alzheimer's disease (AD). Here we report the therapeutic effect of
Guiqin Chen et al.
Science advances, 7(16) (2021-04-18)
Netrin-1, a family member of laminin-related secreted proteins, mediates axon guidance and cell migration during neural development. T835M mutation in netrin receptor UNC5C predisposes to the late-onset Alzheimer's disease (AD) and increases neuronal cell death. However, it remains unclear how

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