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LY 450139

Cat. No. 6559 Submit a Review Datasheet / COA / SDS
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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 (2)
Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for LY 450139

LY 450139 is a 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.

Compound Libraries for LY 450139

LY 450139 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for LY 450139

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 for LY 450139

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

Preparing Stock Solutions for LY 450139

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.

Select a batch to recalculate based on the batch molecular weight:
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 for LY 450139

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

If you know of a relevant reference for LY 450139, please let us know.

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Citations for LY 450139

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