DAPT

Hersteller MedChem Express
Kategorie
Typ Inhibitors
Specific against other
Clon N/A
Menge 5mg
ArtNr HY-13027-5mg
Eclass 6.1 30220300
Eclass 9.0 32160605
Lieferbar
Synonyms
GSI-IX, GSI IX
CAS No.
208255-80-5
Purity
>98%
MW
4324604
Formula
C23H26F2N2O4
Solubility
DMSO: >= 215 mg/mL
Biological Description
DAPT is a gamma-secretase inhibitor, reduces the total beta-amyloid peptide (Abeta) production with IC50 of 20 nM in HEK 293 cells.

IC50 & Target: IC50: 20 nM (Abeta, in HEK 293 cells)[1]
In Vitro: DAPT inhibits Abeta production over 90%, effects only a modest reduction in APPbeta in the culture media. Although APPbeta is reduced by about 30% by DAPT treatment, this effect is not concentration-dependent and is reversed by the removal of DAPT[1]. CNE-2 cells are treated with increasing concentrations of DAPT (0, 25, 50 and 75 uM), and the gamma-secretase-generated Notch 1 fragment Val1744-NICD is decreased after 48 h in a dose-dependent manner (P<0.01). The activation of gamma-secretase is almost completely inhibited by DAPT at the concentration of 50 uM[2].
In Vivo: DAPT is administered to PDAPP mice (100 mg/kg s.c.) and the levels of DAPT and Abeta are examined in the brain cortex. Peak DAPT levels of 490 ng/g are achieved in the brain 3 h after treatment, and levels greater than 100 ng/g (ca.200 nM) are sustained throughout the first 18 h. These brain concentrations of DAPT are in excess of its IC50 for lowering Abeta in neuronal cultures (115 nM), and results in a robust and sustains pharmacodynamic effect[1]. DAPT protects brain against cerebral ischemia by down-regulating the expression of Notch 1 and Nuclear factor kappa B in rats. Western blot analyses also show a significant decrease of Notch 1 and NF-kappaB expression in DAPT (0.03 mg/kg) group (P<0.05 vs. MCAO group)[3].
Publications
Hepatology. 2016 Jul; 64(1):175-88.
J Allergy Clin Immunol. 2016 Jul 16. pii: S0091-6749(16)30629-7.
Free  Sample
Available in quantities of 0, 5mg-1mg. Three different samples per customer per year!
Menge: 5mg
Lieferbar: In stock
Listenpreis: 115,36 €
Preis: 115,36 €
lieferbar

Angebot anfordern

Fragen zum Produkt?

Ihr Ansprechpartner:

Arne Pelz

sales@hoelzel.de

Schließen