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ELND 006

ELND 006 (Compound 30) is a metabolically stable γ-secretase inhibitor designed to selectively inhibit amyloid beta (Aβ) generation while sparing Notch signaling. It was developed through a synthetic strategy emphasizing diversity and chirality. ELND 006, along with its analog ELND007 (Compound 34), progressed into human clinical trials. In preclinical studies, both compounds demonstrated effective reduction of Aβ levels in vitro and in vivo. Comparisons with other γ-secretase inhibitors like Semagacestat, Begacestat, and Avagacestat underscored their potency and specificity in lowering Aβ levels in cerebrospinal fluid (CSF) of healthy human volunteers, suggesting potential therapeutic efficacy in Alzheimer's disease[1].

Product Specifications

CAS Number

[1333990-84-3]

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-006.html

Purity

99.7

Solubility

DMSO : 50 mg/mL (ultrasonic; warming)

Smiles

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

Molecular Formula

C20H14F5N3O2S

Molecular Weight

455.40

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

Shipping Conditions

Blue Ice

Storage Conditions

-20°C (Powder, sealed storage, away from moisture)

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Curated Selection

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