[(2R,4R,5S)-2-ベンジル-5-(BOC-アミノ)-4-ヒドロキシ-6-フェニル-ヘキサノイル]-LEU-PHE-NH2

[(2R,4R,5S)-2-ベンジル-5-(BOC-アミノ)-4-ヒドロキシ-6-フェニル-ヘキサノイル]-LEU-PHE-NH2 価格

[(2R,4R,5S)-2-ベンジル-5-(BOC-アミノ)-4-ヒドロキシ-6-フェニル-ヘキサノイル]-LEU-PHE-NH2 化学特性,用途語,生産方法

• 外観

  白色〜わずかにうすい黄色, 結晶〜粉末又は塊

• 溶解性

  DMSO　>10 mg/mL

• 使用

  N-[(2R,4R,5S)-5-[[(1,1-Dimethylethoxy)carbonyl]amino]-4-hydroxy-1-oxo-6-phenyl-2-(phenylmethyl)hexyl]-L-leucyl-L-phenylalaninamide, is a γ-Secretase Inhibitor, the enzyme complex that catalyzes the cleavage of the amyloid precursor protein (APP) to generate amyloid β-peptide (Aβ), the major causative agent in Alzheimer disease (AD).

• 生物活性

  Potent and selective γ -secretase inhibitor (IC 50 = 17 nM) that displays > 50-fold selectivity over a range of aspartyl, serine and cysteine proteases. Exhibits equal potency for inhibition of A β 40 and A β 42 peptides (IC 50 values are 48 and 67 nM respectively in human neuroblastoma cells). Also regulates CXCR4 and VEGFR2 expression through inhibition of Notch signaling in vitro .

• Biochem/physiol Actions

  L-685,458 mimics the transition state in aspartyl protease. It possesses an IC50 of 17nM with respect to inhibition of Aβ synthesis. It is known to block Notch (neurogenic locus notch homolog protein) signaling, which in turn reduces ERK (extracellular signal regulated kinase) phosphorylation by EGF (epidermal growth factor). L-685,458 targets the active site and substrate binding site of the enzyme.

[(2R,4R,5S)-2-ベンジル-5-(BOC-アミノ)-4-ヒドロキシ-6-フェニル-ヘキサノイル]-LEU-PHE-NH2 生産企業

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[(2R,4R,5S)-2-ベンジル-5-(BOC-アミノ)-4-ヒドロキシ-6-フェニル-ヘキサノイル]-LEU-PHE-NH2 スペクトルデータ(¹HNMR)