2. Apoptosis Neuronal Signaling
  3. Caspase Amyloid-β
  4. 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.

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δ-Secretase inhibitor 11 Chemical Structure

δ-Secretase inhibitor 11 Chemical Structure

CAS No. : 842964-18-5

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Based on 1 publication(s) in Google Scholar

δ-Secretase inhibitor 11 Related Antibodies

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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].

IC50 & 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

δ-Secretase inhibitor 11 Related Antibodies
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

220.23

Formula

C10H12N4O2
CAS No.
Appearance

Solid

Color

Brown to reddish brown

SMILES

NC1=CC=C(N2CCOCC2)C3=NON=C31
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (567.59 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.5407 mL 22.7035 mL 45.4071 mL
5 mM 0.9081 mL 4.5407 mL 9.0814 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 4.5407 mL 22.7035 mL 45.4071 mL 113.5177 mL
5 mM 0.9081 mL 4.5407 mL 9.0814 mL 22.7035 mL
10 mM 0.4541 mL 2.2704 mL 4.5407 mL 11.3518 mL
15 mM 0.3027 mL 1.5136 mL 3.0271 mL 7.5678 mL
20 mM 0.2270 mL 1.1352 mL 2.2704 mL 5.6759 mL
25 mM 0.1816 mL 0.9081 mL 1.8163 mL 4.5407 mL
30 mM 0.1514 mL 0.7568 mL 1.5136 mL 3.7839 mL
40 mM 0.1135 mL 0.5676 mL 1.1352 mL 2.8379 mL
50 mM 0.0908 mL 0.4541 mL 0.9081 mL 2.2704 mL
60 mM 0.0757 mL 0.3784 mL 0.7568 mL 1.8920 mL
80 mM 0.0568 mL 0.2838 mL 0.5676 mL 1.4190 mL
100 mM 0.0454 mL 0.2270 mL 0.4541 mL 1.1352 mL
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δ-Secretase inhibitor 11 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

δ-Secretase inhibitor 11842964-18-5CaspaseAmyloid-ββ-amyloid peptideAβAbetaPala cellsCNS diseasesasparagine endopeptidaseAEPamyloid precursor proteinAPPAlzheimer's diseaseoxygen-glucose deprivationInhibitorinhibitorinhibit

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