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Merck

SML3144

delta-Secretase inhibitor, CP11

≥95% (HPLC)

동의어(들):

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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크기 선택

제품정보 (DICE 배송 시 비용 별도)

실험식(Hill 표기법):
C10H12N4O2
CAS 번호:
842964-18-5
Molecular Weight:
220.23
UNSPSC Code:
12352200
NACRES:
NA.28
MDL number:
MFCD03422529

주요 문서

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도움 문의

SMILES string

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 key

LWCSTSZSZFUHAT-UHFFFAOYSA-N

assay

≥95% (HPLC)

form

powder

color

, Faint Brown to dark red

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

Quality Level

100

Biochem/physiol Actions

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).

pictograms

Skull and crossbones
GHS06

signalword

Danger

hcodes

H302,H311

Hazard Classifications

Acute Tox. 3 Dermal - Acute Tox. 4 Oral

저장 등급

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

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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시험 성적서(COA)

Lot/Batch Number
0000187269
0000187267
0000182497
0000187269
0000187267

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문서 라이브러리 방문

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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