ELN318463 racemate 是 ELN318463 的外消旋体。ELN318463 是淀粉样前体蛋白 (APP) 选择性的 γ-分泌酶 (γ-secretase) 抑制剂。ELN318463 对包含早老蛋白 (PS1) 和 PS2 的 γ-分泌酶抑制活性不同，对 PS1 和 PS2 的 EC50 分别为 12 nM 和 656 nM。ELN318463 对 PS1 的选择性比对 PS2 高约 51 倍。
| 生物活性 |
ELN318463 racemate is the racemate of ELN318463. ELN318463 is an amyloid precursor protein (APP) selective γ-secretase inhibitor. ELN318463 shows differential inhibition of presenilin (PS1)- and PS2-comprised γ-secretase with EC50s of 12nM and 656 nM for PS1and PS2, respectively. ELN318463 is 51-fold more selective for PS1. |
|---|---|
| 体外研究 |
ELN318463 behaves as a classic γ-secretase inhibitor, demonstrates 75- to 120-fold selectivity for inhibiting Aβ production compared with Notch signaling in cells, and displaces an active site directed inhibitor at very high concentrations only in the presence of substrate. |
| 体内研究 |
Brain levels of ELN318463 at 30 mg/kg are 0.754 μM in FVB brains and 0.69 μM in PDAPP brains, and at 100 mg/kg dose the levels were 2.7 μM in FVB brains and 1.87 μM in PDAPP brains. Discordance between Aβ1-40 and Aβx-40 in BACE KO or wild-type BACE inhibitor treated mice has been reported.
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| 分子式 |
C19H20BrClN2O3S
|
| 分子量 |
471.80
|
| CAS号 |
851599-82-1
|
| 运输条件 |
Room temperature in continental US; may vary elsewhere. |
| 储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis. |
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Data Sheet