产品说明
生化/生理作用
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).
基本信息
经验(实验)分子式 | C20H14F5N3O2S |
分子量 | 455.40 |
MDL编号 | MFCD28386354 |
产品性质
测定 | ≥98% (HPLC) |
形式 | powder |
旋光性 | [α]/D -125 to -140°, c = 0.5 in ethanol |
颜色 | white to beige |
溶解性 | DMSO: 2 mg/mL, clear |
储存温度 | 2-8℃ |
安全信息
储存分类代码 | 13 - Non Combustible Solids |
WGK | WGK 3 |