LY 450139

Name: LY 450139
Brand: Tocris Bioscience
SKU: 6559

Tocris Bioscience, part of Bio-Techne | Catalog # 6559

COA / SDS

γ-secretase pseudo-inhibitor

Key Product Details

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)
Molecular Weight:	361.44

View Full Technical Details for LY 450139

Technical Data
Citations

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 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.

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.

Lin Gamma-secretase inhibitors attenuate neurotrauma and neurogenic acute lung injury in rats by rescuing the accumulation of hypertrophic microglia. Cell Physiol.Biochem. 2017 PMID: 29227981
Lanz Concentration-dependent modulation of amyloid-beta in vivo and in vitro using the gamma-secretase inhibitor, LY-450139. J.Pharmacol.Exp.Ther. 2006 PMID: 16920992
Tagami Semagacestat is a pseudo-inhibitor of γ-secretase. Cell Rep. 2017 PMID: 28978478
Henley Development of semagacestat (LY450139), a functional gamma-secretase inhibitor, for the treatment of Alzheimer's disease. Expert Opin.Pharmacother. 2009 PMID: 19527190