344355
AS1842856
≥98% (HPLC), solid, Foxo1 inhibitor, Calbiochem®
Synonyme(s) :
Foxo1 Inhibitor, AS1842856, 5-Amino-7-(cyclohexylamino)-1-ethyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
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About This Item
Formule empirique (notation de Hill):
C18H22FN3O3
Numéro CAS:
Poids moléculaire :
347.38
Numéro MDL:
Code UNSPSC :
12352200
Nomenclature NACRES :
NA.77
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product name
Foxo1 Inhibitor, AS1842856, Foxo1 Inhibitor, AS1842856, is a cell-permeable inhibitor that blocks the transcription activity of Foxo1 (IC₅₀ = 33 nM). Directly binds to the active Foxo1, but not the Ser256-phosphorylated form.
Niveau de qualité
Pureté
≥98% (HPLC)
Forme
solid
Fabricant/nom de marque
Calbiochem®
Conditions de stockage
OK to freeze
protect from light
Couleur
off-white to tan
tan to yellow
Solubilité
DMSO: 5 mg/mL
Conditions d'expédition
ambient
Température de stockage
2-8°C
Chaîne SMILES
O=C1C(C(O)=O)=CN(C2=C1C(N)=C(F)C(NC3CCCCC3)=C2)CC
Description générale
A cell-permeable oxodihydroquinoline that preferentially inhibits the transcription activity of Forkhead box O family member Foxo1 (IC50 = 33 nM) over that of the functionally related Foxo3a and Foxo4 (70%, 20%, and 3% inhibition, respectively, in HepG2-based reporter assays; [AS184256] = 100 nM) via direct binding of the active Foxo1, but not the Ser256-phosphorylated/inactive form of Foxo1. Shown to inhibit gluconeogenesis in rat heptoma Fao cultures (IC50 = 43 nM against glucose production) in vitro and in liver of both non-diabetic and diabetic mice during a 26-hour fasting period (100 mg/kg/8 h p.o.) in vivo. Also available as a 50 mM solution in DMSO (Cat. No. 506081).
A cell-permeable oxodihydroquinoline that preferentially inhibits the transcription activity of Forkhead box O family member Foxo1 over that of the functionally related Foxo3a and Foxo4 (70%, 20%, and 3% inhibition, respectively, in HepG2-based reporter assays; [AS184256] = 100 nM) in a dose-dependent manner (IC50 = 33 nM) via direct binding of the non-Ser256-phosphorylated/active Foxo1, but not the Ser256-phosphorylated/inactive form of Foxo1. Shown to inhibit gluconeogenesis in rat heptoma Fao cultures (IC50 = 37 and 130 nM against PEPCK and G6Pase mRNA level; IC50 = 43 nM against glucose production) in vitro and in murine liver of both normoglycemic ICR mice (60% and 45% inhibition of hepatic G6Pase and PEPCK mRNA level, respectively; three 100 mg/kg p.o. dosages at 0, 12, 24 h) and diabetic db/db mice (86%, 70%, 56%, 48%, 35%, and 31% inhibition of hepatic G6Pase, ABCG8, ABCG5, PEPCK, IL-1β, and apoCIII mRNA level, respectively; three 100 mg/kg p.o. dosages at 0, 12, 24 h) during a 26-hour fasting period in vivo.
Conditionnement
Packaged under inert gas
Avertissement
Toxicity: Regulatory Review (Z)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Autres remarques
Nagashima, T., et al. 2010. Mol. Pharmacol.78, 961.
Informations légales
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Code de la classe de stockage
11 - Combustible Solids
Classe de danger pour l'eau (WGK)
WGK 1
Point d'éclair (°F)
Not applicable
Point d'éclair (°C)
Not applicable
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