LY-411575 isomer 3__DataSheet_MedChemExpress

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Product Name:
LY-411575 isomer 3
CAS No.:
Cat. No.:
HY-50752C Product Data Sheet
MWt:
479.48Formula:
C26H23F2N3O4Purity :>98%Solubility:
DMSO
Mechanisms:
Biological Activity:
LY-411575isomer 3is a isomer of LY411575which is a potent -secretase inhibitor with IC50of
Pathways:Neuronal Signaling; Target:γ-secretase LY-411575 isomer 3 is a isomer of LY411575, which is a potent γ-secretase inhibitor with IC50 of 0.078 nM/0.082 nM (membrane/cell-based), also inhibits Notch clevage with withIC50 of 0.39 nM.
IC50 value: 0.078 nM/0.082 nM (membrane/cell-based) [1]
Target: γ-secretase in vitro: LY-411575 inhibits γ-secretase which can be assessed by the substrates like amyloid precursor protein (APP) and Notch S3 cleavage [1]. LY-411575, which blocks Notch activation,
results in apoptosis in primary and immortalized KS cells [2].in vivo: 10 mg/kg oral dose of LY-411575 decreases brain and plasma A β40 and -42 dose-
dependently. [1] LY-411575 reduces cortical A β40 in young (preplaque) transgenic CRND8 mice References:
[1]. Wong GT, et al. Chronic treatment with the gamma-secretase inhibitor LY-411,575 inhibits beta-amyloid peptide production and alters lymphopoiesis and intestinal cell differentiation. J Biol Chem.
2004 Mar 26;279(13):12876-82.(ED50 ≈ 0.6 mg/kg) and produces significant thymus atrophy and intestinal goblet cell hyperplasia at higher doses (>3 mg/kg). The therapeutic window is similar after oral and subcuta...
;()[2]. Curry CL, et al. Gamma secretase inhibitor blocks Notch activation and induces apoptosis in
Kaposi's sarcoma tumor cells. Oncogene. 2005 Sep 22;24(42):6333-44.[3]. Hyde LA, et al. Studies to investigate the in vivo therapeutic window of the gamma-secretase inhibitor N2-[(2S)-2-(3,5-difluorophenyl)-2-hydroxyethanoyl]-N1-[(7S)-5-methyl-6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl]-L-alaninamide (LY411,575) in the CRND8 mouse. J Pharmacol Exp Ther.
2006 Dec;319(3):1133-43.Caution: Not fully tested. For research purposes only
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