Semagacestat (LY450139)

Catalog No. A10836

Semagacestat (LY450139)是一种针对Aβ42，Aβ40和Aβ38的γ-分泌酶阻滞剂，IC50分别为10.9 nM，12.1 nM和12.0 nM。 Semagacestat还抑制Notch信号传导，IC50为14.1 nM。

Product Citations

Yesuvadian R, .et al. Potent γ-secretase inhibitors/modulators interact with amyloid-β fibrils but do not inhibit fibrillation: a high-resolution NMR study., Biochem Biophys Res Commun., 2014, May 16;447(4):590-5 PMID: 24747079

Technical details

Catalog Num	A10836
M. Wt	361.4
Formula	C19H27N3O4
Purity	>98%
Storage	at -20°C 3 years Powder
CAS No.	425386-60-3
Synonyms	LY-450139
SMILES	C[C@@H](C(=O)N[C@H]1C2=CC=CC=C2CCN(C1=O)C)NC(=O)[C@H](C(C)C)O

Biological Activity

Semagacestat (LY450139)是一种针对Aβ42，Aβ40和Aβ38的γ-分泌酶阻滞剂，IC50分别为10.9 nM，12.1 nM和12.0 nM。 Semagacestat还抑制Notch信号传导，IC50为14.1 nM。

Targets

γ secretase(Aβ42) (H4 human glioma cells)	γ secretase(Aβ38) (H4 human glioma cells)	γ secretase(Aβ40) (H4 human glioma cells)	Notch (H4 human glioma cells)
10.9 nM	12.0 nM	12.1 nM	14.1 nM

Solubility *

In vitro (25°C)	DMSO	66 mg/mL (182.6 mM)
	Water	Insoluble
	Ethanol	38 mg/mL (105.13 mM)
In vivo	0.5% methylcellulose	28 mg/mL
* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Preparing Stock Solutions

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.1 mM	27.67 mL	138.35 mL	276.7 mL
0.5 mM	5.53 mL	27.67 mL	55.34 mL
1 mM	2.77 mL	13.84 mL	27.67 mL
5 mM	0.55 mL	2.77 mL	5.53 mL

*The above data is based on the productmolecular weight 361.4 . Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.