δ-Secretase inhibitor 11
Based on 1 publication(s) in Google Scholar
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.
For research use only. We do not sell to patients.
- Purity: 99.89%
- CAS No.: 842964-18-5
- Formula: C10H12N4O2
- Molecular Weight:220.23
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) δ-Secretase inhibitor 11
MoreAll Caspase Isoforms
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Biological Activity
Description
IC50 & Target
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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.
In Vivo
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.
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Animal Model:Tau P301S transgenic mice (n=4 mice per group)[1]
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Dosage:10 mg/kg
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Administration:Orally, once daily for 3 months
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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.
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Animal Model:5XFAD mice[1]
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Dosage:2, 5 or 10 mg kg
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Administration:Orally, once daily for 1.5 and 3 months
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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.
Chemical Information
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CAS No. 842964-18-5
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Appearance Solid
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Molecular Weight 220.23
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Formula C10H12N4O2
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Color Brown to dark brown
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SMILES
NC1=CC=C(N2CCOCC2)C3=NON=C31
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (1)
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Journal Impact Factor
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Most Recent
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Brain Behav Immun
2024 Jul:119:56-83. PMID: 38555992
Solvent & Solubility
In Vitro:
DMSO : 116.67 mg/mL (529.76 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (275 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
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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