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[1].

Product Specifications

CAS Number

[1444006-79-4]

UNSPSC

12352005

Target

Amyloid-β; γ-secretase

Type

Reference compound

Related Pathways

Neuronal Signaling; Stem Cell/Wnt

Applications

Metabolism-protein/nucleotide metabolism

Field of Research

Metabolic Disease

Assay Protocol

https://www.medchemexpress.com/elnd-007.html

Smiles

O=S(N1[C@H](C2CC2)C3=CNN=C3C4=C1C=CC(F)=C4)(C5=CC=C(C(F)(F)F)N=C5)=O

Molecular Formula

C19H14F4N4O2S

Molecular Weight

438.40

References & Citations

[1]Discovery of (R) -4-Cyclopropyl-7,8-difluoro-5- (4- (trifluoromethyl) phenylsulfonyl) -4,5-dihydro-1H-pyrazolo[4,3-c]quinoline (ELND006) and (R) -4-Cyclopropyl-8-fluoro-5- (6- (trifluoromethyl) pyridin-3-ylsulfonyl) -4,5-dihydro-2H-pyrazolo[4,3-c]quinoline (ELND007) : Metabolically Stable γ-Secretase Inhibitors that Selectively Inhibit the Production of Amyloid-β over Notch