产品
编 号：F480073
分子式：C19H20BrClN2O3S
分子量：471.8
分子式：C19H20BrClN2O3S
分子量：471.8
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CAS No: 851599-82-1
产品详情
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.
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.
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.
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.
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