SML2122

ELND006

≥98% (HPLC)

• Synonym(e): (R)-4-Cyclopropyl-7,8-difluoro-5-(4-(trifluoromethyl)phenylsulfonyl)-4,5-dihydro-1H-pyrazolo[4,3-c]quinoline
• Empirische Formel (Hill-System): C₂₀H₁₄F₅N₃O₂S
• CAS-Nummer: 1333990-84-3
• Molekulargewicht: 455.40
• UNSPSC Code: 12352200
• NACRES: NA.77
• MDL number: MFCD28386354
• Assay: ≥98% (HPLC)
• Form: powder

Eigenschaften

• assay: ≥98% (HPLC)
• form: powder
• optical activity: [α]/D -125 to -140°, c = 0.5 in ethanol
• color: white to beige
• solubility: DMSO: 2 mg/mL, clear
• storage temp.: 2-8°C

Beschreibung

Biochem/physiol Actions

ELND006 is an allosteric γ-secretase inhibitor that selectively blocks amyloid-β (Aβ) over Notch production both in cell-free (Aβ IC50/Notch IC50 = 0.34 nM/6.6 nM) and cell-based assays (Aβ IC50/Notch IC50 = 1.3 nM/85 nM). ELND006 is orally available and blood-brain barrier-permeable (total/unbound conc in brain = 0.12 μM/1.0 nM, 0.52 μM/4.5 nM, 2.1 μM/18 nM and total/unbound conc in plasma = 0.031 μM/0.28 nM, 0.19 μM/1.7 nM, 0.90 μM/8.1 nM 3 h post 1, 3, 10 mg/kg oral dosage in rats, respectively), and shown to effectively reduce cortical Aβx-40 in mice in vivo (by 32%, 48%, and 61% 3 h post 1, 3, 10 mg/kg oral dosage).

Orally active allosteric γ-secretase inhibitor that selectively inhibits the production of amyloid-β (Aβ) over Notch with brain Aβx-40-lowering efficacy in vivo.

Sicherheitshinweise

• Lagerklasse: 11 - Combustible Solids
• wgk: WGK 3