SML3144
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
推薦產品
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
SMILES 字串
N3(CCOCC3)c1c2n[o]nc2c(cc1)N
InChI
1S/C10H12N4O2/c11-7-1-2-8(10-9(7)12-16-13-10)14-3-5-15-6-4-14/h1-2H,3-6,11H2
InChI 密鑰
LWCSTSZSZFUHAT-UHFFFAOYSA-N
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.
Orally active, brain-penetrant, selective delta-secretase (δ-secretase; AEP) inhibitor that improves cognitive functions in murine models of Alzheimer′s disease (AD).
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
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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