ELND 007
ELND 007 (Compound 34) is a metabolically stable γ-secretase inhibitor designed to selectively inhibit amyloid beta (Aβ) generation while minimizing Notch inhibition. Developed alongside ELND 006 (Compound 30), it underwent human clinical trials following a synthetic strategy emphasizing diversity and chirality. In preclinical studies, ELND 007 showed promising in vitro and in vivo characteristics, effectively reducing Aβ levels. Comparative studies with other γ-secretase inhibitors like Semagacestat, Begacestat, and Avagacestat highlighted its efficacy in lowering Aβ production, particularly demonstrated by reduced Aβ levels in the cerebrospinal fluid (CSF) of healthy human volunteers, suggesting potential therapeutic benefit for Alzheimer's disease.
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- CAS No.: 1444006-79-4
- Formule: C19H14F4N4O2S
- Masse moléculaire:438.40
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | ED50 |
0.28 nM
Compound: 34, ELND007
|
Inhibition of gamma-secretase in CHO cells assessed expressing APPSw assessed as inhibition of amyloid beta(1 to x) secretion after overnight incubation by ELISA
Inhibition of gamma-secretase in CHO cells assessed expressing APPSw assessed as inhibition of amyloid beta(1 to x) secretion after overnight incubation by ELISA
|
[PMID: 23713656] |
| CHO | ED50 |
20 nM
Compound: 34, ELND007
|
Inhibition of gamma-secretase in CHO cells assessed expressing NotchdeltaE assessed as inhibition of notch cleavage after overnight incubation by luciferase reporter gene assay
Inhibition of gamma-secretase in CHO cells assessed expressing NotchdeltaE assessed as inhibition of notch cleavage after overnight incubation by luciferase reporter gene assay
|
[PMID: 23713656] |
Chemical Information
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CAS No. 1444006-79-4
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Masse moléculaire 438.40
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Formule C19H14F4N4O2S
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SMILES
O=S(N1[C@H](C2CC2)C3=CNN=C3C4=C1C=CC(F)=C4)(C5=CC=C(C(F)(F)F)N=C5)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)