| Identification | Back Directory | [Name]
ELND 006 | [CAS]
1333990-84-3 | [Synonyms]
ELND 006
ELND0006
ELND006 >=98% (HPLC)
2H-Pyrazolo[4,3-c]quinoline, 4-cyclopropyl-7,8-difluoro-4,5-dihydro-5-[[4-(trifluoromethyl)phenyl]sulfonyl]-, (4R)- | [Molecular Formula]
C20H14F5N3O2S | [MDL Number]
MFCD28386354 | [MOL File]
1333990-84-3.mol | [Molecular Weight]
455.4 |
| Chemical Properties | Back Directory | [storage temp. ]
2-8°C | [solubility ]
DMSO: 2mg/mL, clear | [form ]
powder | [color ]
white to beige | [Optical Rotation]
[α]/D -125 to -140°, c = 0.5 in ethanol |
| Hazard Information | Back Directory | [Biological Activity]
ELND006 is an allosteric γ-secretase inhibitor th at 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 nM0.52 μM/4.5 nM2.1 μM/18 nM and total/unbound conc in plasma = 0.031 μM/0.28 nM0.19 μM/1.7 nM0.90 μM/8.1 nM 3 h post 1310 mg/kg oral dosage in ratsrespectively)and shown to effectively reduce cortical Aβx-40 in mice in vivo (by 32%48%and 61% 3 h post 1310 mg/kg oral dosage). |
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| Company Name: |
SPIRO PHARMA
|
| Tel: |
|
| Website: |
www.spiropharma.com.cn |
| Company Name: |
Energy Chemical
|
| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
| Company Name: |
Merck KGaA
|
| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
|