产品属性：
产品名称 | 规格 | CAS号 | 型号 |
ELN 318463 racemate | 1mg 5mg 10mg 20mg | 851599-82-1 | EY-Y0164686 |
Cas No.851599-82-1
别名 N/A
化学名 N/A
分子式 C19H20BrClN2O3S
分子量 471.8
溶解度 Soluble in DMSO
储存条件 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
产品描述：
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.
关键字： 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.主要从事免疫学、分子生物学和常规生化试剂等为一体的科研产品销售企业，公司自成立以来，秉承""全心全意服务于科研工作者""的企业理念，立足生物科技领域，运用生物技术和科研试剂，发展现代生物科技，为各类大中小医院及其它医疗机构、高等院校、科研院所、企事业单位提供优质的产品，服务生物科技领域的科学研究人员。
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