L-685,458|γ-secretase inhibitor|DC Chemicals

L-685,458|γ-secretase inhibitor|DC Chemicals

L-685,458 is a selective and Potent inhibitor of γ-secretase with IC50 value of 17 nM.

Product Name: L-685,458 |Catalog Number: DC8615 |CAS 292632-98-5 |Other names: L-685458,L 685458，L685458 |Chemical Name: tert-butyl N-[(2S,3R,5R)-6-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-benzyl-3-hydroxy-6-oxo-1-phenylhexan-2-yl]carbamate |Molecule Formular: C39H52N4O6 |MW: 672.85

L-685,458 is a transition state analogue inhibitor.

It is a pan-inhibitor of γ-secretase which decrease the products of Aβ(42) and Aβ(40) peptides. It displays a selectivity of 50-fold or greater inhibition than a range of aspartyl, serine, and cysteine protease in vitro membrane assay. L-685,458 reduced the product both total Aβand Aβ42 in human primary neuronal cells with IC50 value of 115 nM for Aβand Aβ42 for 200 nM[2]. L-685,458 also inhibitedγ-secretase activity by characterizing the production of total secreted Aβby ELISA with IC50 value of about 5 nM in HEK 293 cells overexpressing human APP751.

L-685,458 reduced the cortical total Aβwith a 50% reduction occurring at 100 mg/kg in a dose-dependent manner in PDAPP, and similar reductions in cortical Aβ42 were observed. L-685,458 decreased brain levels of Aβwhen given orally to Tg2576 mice that are transgenic for human APPV717F mutation. [3] L-685,458 also inhibit the Notch signaling, then affects embryonic development in zebrafish embryos.

For research and scientific purpose only, not for human use.