產品屬性：
產品名稱 | 規(guī)格 | CAS號 | 型號 |
ELN 318463 racemate | 1mg 5mg 10mg 20mg | 851599-82-1 | EY-Y0164686 |
Cas No.851599-82-1
別名 N/A
化學名 N/A
分子式 C19H20BrClN2O3S
分子量 471.8
溶解度 Soluble in DMSO
儲存條件 Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
產品描述：
ELN 318463 racemate is the racemate of ELN 318463. ELN 318463 is a selective gamma-secretase inhibitor.
The amyloid precursor protein (APP) selective gamma-secretase inhibitors ELN318463 and ELN475516 reported here behave as classic gamma-secretase inhibitors, demonstrate 75- to 120-fold selectivity for inhibiting Aβ production compared with Notch signaling in cells, and displace an active site directed inhibitor at very high concentrations only in the presence of substrate. ELN318463 demonstrates discordant efficacy for reduction of brain Aβ in the PDAPP compared with wild-type FVB. In the presence of 1 Km (20 μg/mL) MBP-C125 substrate, ELN318463 is able to displace the active site isostere at an ED50 of 23 μM. These values represent an approximately 2,000X and 67X multiple over the IC50 values of the two compounds in the gammaAPP assay[1].
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[1].
[1]. Basi GS, et al. Amyloid precursor protein selective gamma-secretase inhibitors for treatment of Alzheimer's disease. Alzheimers Res Ther. 2010 Dec 29;2(6):36.
關鍵字： 851599-82-1;C19H20BrClN2O3S;ELN 318463 racemate;
上海一研生物科技有限公司Shanghai yiyan bio-technology Co. Ltd.主要從事免疫學、分子生物學和常規(guī)生化試劑等為一體的科研產品銷售企業(yè)，公司自成立以來，秉承""全心全意服務于科研工作者""的企業(yè)理念，立足生物科技領域，運用生物技術和科研試劑，發(fā)展現(xiàn)代生物科技，為各類大中小醫(yī)院及其它醫(yī)療機構、高等院校、科研院所、企事業(yè)單位提供優(yōu)質的產品，服務生物科技領域的科學研究人員。
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