344355

AS1842856

≥98% (HPLC), solid, Foxo1 inhibitor, Calbiochem^®

• Szinonimák: Foxo1 Inhibitor, AS1842856, 5-Amino-7-(cyclohexylamino)-1-ethyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
• Tapasztalati képlet (Hill-képlet): C₁₈H₂₂FN₃O₃
• CAS-szám: 836620-48-5
• Molekulatömeg: 347.38
• MDL-szám: MFCD30718173
• UNSPSC kód: 12352200
• NACRES: NA.77

Tulajdonságok

• Terméknév: 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.
• Minőségi szint: 100
• Teszt: ≥98% (HPLC)
• Forma: solid
• gyártó/kereskedő neve: Calbiochem^®
• tárolási körülmény: OK to freeze; protect from light
• szín: off-white to tan; tan to yellow
• oldhatóság: DMSO: 5 mg/mL
• kiszállítva: ambient
• tárolási hőmérséklet: 2-8°C
• SMILES string: O=C1C(C(O)=O)=CN(C2=C1C(N)=C(F)C(NC3CCCCC3)=C2)CC
• InChI: 1S/C18H22FN3O3/c1-2-22-9-11(18(24)25)17(23)14-13(22)8-12(15(19)16(14)20)21-10-6-4-3-5-7-10/h8-10,21H,2-7,20H2,1H3,(H,24,25)

Leírás

Általános leírás

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.

Kiszerelés

Packaged under inert gas

Figyelmeztetés

Toxicity: Regulatory Review (Z)

Feloldás

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Egyéb megjegyzések

Nagashima, T., et al. 2010. Mol. Pharmacol.78, 961.

Jogi információk

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Biztonsági adatok

• Tárolási osztály kódja: 11 - Combustible Solids
• WGK: WGK 1
• Lobbanási pont (F): Not applicable
• Lobbanási pont (C): Not applicable