Synonym: (R)-4-Cyclopropyl-7,8-difluoro-5-(4-(trifluoromethyl)phenylsulfonyl)-4,5-dihydro-1H-pyrazolo[4,3-c]quinoline
CAS Number: 1333990-84-3
Empirical Formula (Hill Notation): C20H14F5N3O2S
Molecular Weight: 455.40
MDL Number: MFCD28386354
Linear Formula: C20H14F5N3O2S
Product Type: Chemical
assay |
≥98% (HPLC) |
color |
white to beige |
form |
powder |
optical activity |
[α]/D -125 to -140°, c = 0.5 in ethanol |
solubility |
DMSO: 2 mg/mL, clear |
storage temp. |
2-8°C |
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). |
RIDADR |
NONH for all modes of transport |
WGK Germany |
WGK 3 |
Purity |
≥98% (HPLC) |
Storage Temp. |
2-8°C |
UNSPSC |
12352200 |