Compound 11

Catalog No.E0363 Batch:E036301

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Technical Data

Formula

C10H12N4O2
Molecular Weight 220.23 CAS No. 842964-18-5
Solubility (25°C)* In vitro DMSO 44 mg/mL (199.79 mM)
Ethanol 4 mg/mL (18.16 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description 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.
Targets
Secretase [1]
(in fluorescence-based assay)		 δ-secretase [1]
(in Pala cells assay)
0.7 μM 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.[1]
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.[2]

Protocol (from reference)

Cell Assay:

[1]
  • Cell lines

    Pala cells, HepG2 cells

  • Concentrations

    24 h

  • Incubation Time

    50 μM

  • Method

    Cells are incubated with various concentrations of compound 11 with the Pala cells for 2 h at 37 °C. Cells are collected, washed twice with PBS and lysed in Lysis Buffer. The protein concentrations are normalized via a Bradford assay and lysates are assayed with 5 μM Cbz-Ala-Ala-Asn-AMC.
Animal Study:

[2]
  • Animal Models

    senescence-accelerated mouse prone 8 (SAMP8) mice

  • Dosages

    10 mg/kg

  • Administration

    o.g.

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.