δ-secretase inhibitor 11

Modify Date: 2024-01-29 06:55:06

δ-secretase inhibitor 11 Structure
δ-secretase inhibitor 11 structure
Common Name δ-secretase inhibitor 11
CAS Number 842964-18-5 Molecular Weight 220.22800
Density N/A Boiling Point N/A
Molecular Formula C10H12N4O2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of δ-secretase inhibitor 11


δ-Secretase inhibitor 11 (compound 11) is an orally active, potent, BBB-penetrated, non-toxic, selective and specific δ-secretase inhibitor, with an IC50 of 0.7 μM. δ-Secretase inhibitor 11 interacts with both the active site and allosteric site of δ-secretase. δ-Secretase inhibitor 11 attenuates tau and APP (amyloid precursor protein) cleavage. δ-Secretase inhibitor 11 ameliorates synaptic dysfunction and cognitive impairments in tau P301S and 5XFAD transgenic mouse models. δ-Secretase inhibitor 11 can be used for Alzheimer's disease research[1].

 Names

Name 7-Morpholin-4-yl-benzo[1,2,5]oxadiazol-4-ylamine
Synonym More Synonyms

 δ-secretase inhibitor 11 Biological Activity

Description δ-Secretase inhibitor 11 (compound 11) is an orally active, potent, BBB-penetrated, non-toxic, selective and specific δ-secretase inhibitor, with an IC50 of 0.7 μM. δ-Secretase inhibitor 11 interacts with both the active site and allosteric site of δ-secretase. δ-Secretase inhibitor 11 attenuates tau and APP (amyloid precursor protein) cleavage. δ-Secretase inhibitor 11 ameliorates synaptic dysfunction and cognitive impairments in tau P301S and 5XFAD transgenic mouse models. δ-Secretase inhibitor 11 can be used for Alzheimer's disease research[1].
Related Catalog
Target

Caspase-3:31.86 ± 1. μM (IC50)

Caspase-8:86.71 ± 10 μM (IC50)

In Vitro δ-Secretase inhibitor 11 (compound 11) (0-1 μM, 10 min) inhibits δ-secretase in a concentration- and time-dependent manner[1]. δ-Secretase inhibitor 11 (0-1 μM) selectively blocks tau and APP (amyloid precursor protein) fragmentation by δ-secretase[1].
In Vivo δ-Secretase inhibitor 11 (compound 11) (10 mg/kg, Orally, once daily for 3 months) attenuates neuronal injury induced by OGD (oxygen-glucose deprivation), and specifically exerts neuroprotective actions[1]. δ-Secretase inhibitor 11 (0-10 mg/kg, Orally, once daily for 1.5 and 3 months) inhibits δ-secretase activity, attenuates Aβ deposition and cognitive deficits in 5XFAD mouse model[1]. Animal Model: Tau P301S transgenic mice (n=4 mice per group)[1] Dosage: 10 mg/kg Administration: Orally, once daily for 3 months Result: Significantly inhibited the activity of δ-secretase in both wild-type and tau P301S mice brain, increased PP2A activity, and attenuated the truncation and phosphorylation of tau in tau P301S mice. Ameliorated synaptic loss and restored synaptic dysfunction in tau P301S mice. Animal Model: 5XFAD mice[1] Dosage: 2, 5 or 10 mg kg Administration: Orally, once daily for 1.5 and 3 months Result: Attenuated the β-secretase-mediated processing of APP, significantly decreased the concentrations of Aβ 1-40 and Aβ 1-42 in the brain lysates, and attenuated Aβ deposition in a time- and dose-dependent manner.
References

[1]. Zhang Z, et al. Inhibition of delta-secretase improves cognitive functions in mouse models of Alzheimer's disease. Nat Commun. 2017 Mar 27;8:14740.

 Chemical & Physical Properties

Molecular Formula C10H12N4O2
Molecular Weight 220.22800
Exact Mass 220.09600
PSA 77.41000
LogP 1.28780

 Safety Information

HS Code 2934999090

 Customs

HS Code 2934999090
Summary 2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

 Synonyms

7-(Methylthio)xanthone-3-carboxamide
9H-Xanthene-3-carboxamide,7-(methylthio)-9-oxo
7-(morpholin-4-yl)-2,1,3-benzoxadiazol-4-amine
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