LY 450139

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Cat.No. 6559 - LY 450139 | C19H27N3O4 | CAS No. 425386-60-3
Description: γ-secretase pseudo-inhibitor
Chemical Name: (2S)-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]butanamide
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature

Biological Activity

γ-secretase pseudo-inhibitor. Inhibits Aβ secretion from cells in vitro and increases accumulation of γ-secretase products and long Aβ species in vitro and in vivo. Also attenuates the accumulation of activated microglia and neurological injury in a traumatic brain injury animal model.

Technical Data

M. Wt 361.44
Formula C19H27N3O4
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 425386-60-3
PubChem ID 9843750
InChI Key PKXWXXPNHIWQHW-RCBQFDQVSA-N
Smiles CC([C@@H](C(N[C@H](C(N[C@H]1C2=CC=CC=C2CCN(C1=O)C)=O)C)=O)O)C

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 36.14 100
ethanol 18.07 50

Preparing Stock Solutions

The following data is based on the product molecular weight 361.44. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.77 mL 13.83 mL 27.67 mL
5 mM 0.55 mL 2.77 mL 5.53 mL
10 mM 0.28 mL 1.38 mL 2.77 mL
50 mM 0.06 mL 0.28 mL 0.55 mL

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References

References are publications that support the biological activity of the product.

Henley et al (2009) Development of semagacestat (LY450139), a functional gamma-secretase inhibitor, for the treatment of Alzheimer's disease. Expert Opin.Pharmacother. 10 1657 PMID: 19527190

Lanz et al (2006) Concentration-dependent modulation of amyloid-beta in vivo and in vitro using the gamma-secretase inhibitor, LY-450139. J.Pharmacol.Exp.Ther. 319 924 PMID: 16920992

Tagami et al (2017) Semagacestat is a pseudo-inhibitor of γ-secretase. Cell Rep. 21 259 PMID: 28978478

Lin et al (2017) Gamma-secretase inhibitors attenuate neurotrauma and neurogenic acute lung injury in rats by rescuing the accumulation of hypertrophic microglia. Cell Physiol.Biochem. 44 1726 PMID: 29227981


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Keywords: LY 450139, LY 450139 supplier, LY450139, Semagacestat, gamma, secretase, inhibitor, inhibits, amyloid, beta, secretion, Abeta, Gamma-Secretase, 6559, Tocris Bioscience

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