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Semagacestat

Chemical Structure : Semagacestat

CAS No.: 425386-60-3

Semagacestat (LY450139;LY-450139)

Catalog No.: PC-42053Not For Human Use, Lab Use Only.

Semagacestat (LY-450139) is a potent γ-secretase inhibitor that inhibits β-amyloid Aβ42, Aβ38 and Aβ40 with IC50 of 10.9, 12 and 12.1 nM, respectively.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Semagacestat (LY-450139) is a potent γ-secretase inhibitor that inhibits β-amyloid Aβ42, Aβ38 and Aβ40 with IC50 of 10.9, 12 and 12.1 nM, respectively.
Semagacestat (LY-450139) reduces the secretion of Aβ42, Aβ40, and Aβ38 in cells and increases β-CTF in cell lysates, also inhibits Notch signaling with IC50 of 14.1 nM.
Semagacestat (LY-450139) increases intracellular byproduct peptides, produced along with Aβ through serial γ-cleavage of βAPP, as well as intracellular long Aβ species, in cell-based and in vivo studies of AD model mice; a pseudo-inhibitor of γ-secretase.

Physicochemical Properties

M.Wt 361.4354
Formula C19H27N3O4
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

Butanamide, 2-hydroxy-3-methyl-N-[(1S)-1-methyl-2-oxo-2-[[(1S)-2,3,4,5-tetrahydro-3-methyl-2-oxo-1H-3-benzazepin-1-yl]amino]ethyl]-, (2S)-

References

1. Lanz TA, et al. J Pharmacol Exp Ther. 2006 Nov;319(2):924-33.

2. Mitani Y, et al. J Neurosci. 2012 Feb 8;32(6):2037-50.

3. Elvang AB, et al. J Neurochem. 2009 Sep;110(5):1377-87.

4. Tagami S, et al. Cell Rep. 2017 Oct 3;21(1):259-273.

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