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β-Secretase Inhibitor IV
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
β-Secretase Inhibitor IV图片
CAS NO:797035-11-1
包装与价格：
包装价格(元)
500μg电议
1mg电议
5mg电议

产品介绍
β-Secretase Inhibitor IV 是一种有效的细胞活性 BACE-1 抑制剂，在 BACE-1 浓度为 2 nM 和 100 pM 下，IC50 分别为 15.6 和 16.3nM。
Cas No.797035-11-1
化学名N1-[(1S,2R)-3-(cyclopropylamino)-2-hydroxy-1-(phenylmethyl)propyl]-5-[methyl(methylsulfonyl)amino]-N3-[(1R)-1-phenylethyl]-1,3-benzenedicarboxamide
Canonical SMILESCN(S(C)(=O)=O)C1=CC(C(N[C@H](C)C2=CC=CC=C2)=O)=CC(C(N[C@@H](CC3=CC=CC=C3)[C@H](O)CNC4CC4)=O)=C1
分子式C31H38N4O5S
分子量578.7
溶解度10mg/mL in ethanol, 20mg/mL in DMSO or in DMF
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

β-Secretase inhibitor IV is an inhibitor of β-site amyloid protein cleaving enzymes (BACE/β-secretase) 1 and 2 (IC50s = 15 and 230 nM for human BACE1 and 2, respectively). [1] It has >500-fold selectivity for BACE1 and 2 over the aspartyl proteases renin and cathepsin D. β-Secretase inhibitor IV inhibits secretion of amyloid-β (Aβ) precursor protein (APP; IC50 = 29 nM) in HEK293T cells transfected with a truncated APP. It also inhibits formation of the Aβ peptides Aβ38, Aβ40, and Aβ42 in primary chick neurons (IC50s = 3.7, 4.7, and 4.8 nM, respectively).[2]

Reference:
[1.] Stachel, S.J., Coburn, C.A., Steele, T.G., et al. Structure-based design of potent and selective cell-permeable inhibitors of human ss-secretase (BACE-1). Journal of Medicinal Chemistry 47(26), 6447-6450 (2004).
[2]. Czvitkovich, S., Duller, S., Mathiesen, E., et al. Comparison of pharmacological modulation of APP metabolism in primary chicken telencephalic neurons and in a human neuroglioma cell line. J. Mol. Neurosci. 43(3), 257-267 (2011).