Home Proteases Secretase inhibitor Compound 11

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Compound 11 Secretase inhibitor

Cat.No.E0363

Compound 11, a non-toxic and selective δ-secretase inhibitor (IC50=0.7 μM, in fluorescence-based assay) that interacts with both the active site and allosteric site of δ-secretase in Co-crystal structure analysis. The IC50 value of the compound 11 towards δ-secretase in Pala cells is 0.8 μM.
Compound 11 Secretase inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 220.23

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Quality Control

Batch: E036301 DMSO]44 mg/mL]false]Ethanol]4 mg/mL]false]Water]Insoluble]false Purity: 99.07%
99.07

Solubility

In vitro
Batch:

DMSO : 44 mg/mL (199.79 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 4 mg/mL

Water : Insoluble

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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight 220.23 Formula

C10H12N4O2

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 842964-18-5 -- Storage of Stock Solutions

Mechanism of Action

Targets/IC50/Ki
Secretase
(in fluorescence-based assay)
0.7 μM
δ-secretase
(in Pala cells assay)
0.8 μM
In vitro

Compound 11 inhibit δ-secretase in Pala cells, with an IC50 of 7 μM. Compounds 11 is highly permeable assessed by Caco-2 monolayer permeability screen. The human liver microsomal stability screen demonstrates that following 30 min of incubation, 76% of compound 11 remained in human liver microsomes.
In vivo

Chronic treatment with δ-secretase inhibitor 11 markedly decreases the brain asparaginyl endopeptidase (AEP) activity, reduces the generation of Aβ1-40/42 and ameliorates memory loss. The inhibition of AEP with this reagent not only reduces the AEP-cleaved tau fragments and tau hyperphosphorylation, but also attenuates neuroinflammation in the form of microglial activation. Treatment with δ-secretase inhibitor 11 prevents the synaptic loss and alleviated dendritic disruption in senescence-accelerated mouse prone 8 (SAMP8) mouse brain.
References

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