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FBPase-IN-1

Katalog-Nr.GC70977

FBPase-IN-1 ist ein starker FBPase (Fructose-1,6-Bisphosphatase)-Inhibitor für die Typ-2-Diabetes-Studie (T2D) mit einem IC50 von 0,22 μM.

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FBPase-IN-1 Chemische Struktur

Cas No.: 20362-54-3

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5 mg
135,00 $
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10 mg
216,00 $
Auf Lager
25 mg
410,00 $
Auf Lager
50 mg
648,00 $
Auf Lager

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Sample solution is provided at 25 µL, 10mM.

Description Chemical Properties Product Documents
FBPase-IN-1 is a potent FBPase (Fructose-1,6-bisphosphatase) inhibitor for Type 2 diabetes (T2D) study with an IC50 of 0.22 μM. FBPase-IN-1 can reduce blood glucose levels and ameliorate glucose tolerance. FBPase-IN-1 modifies the C128 site, regulates the N125-S124-S123 allosteric pathway of FBPase and affects the catalytic activity of FBPase.

FBPase-IN-1 (compund 3a) (1.5625-200 μM, 48 hours) shows a low cytotoxicity with an IC50 of 75.08 μM[1].
FBPase-IN-1 (0-45 min) inhibits FBPase in a time-dependent manner, with IC50 decreasing from 0.28 to 0.09 μM, shows FBPase-IN-1 is an irreversible covalent inhibitor of FBPase[1].

FBPase-IN-1 (12 h-fasted ICR mouse, n = 6, male, 25 mg/kg, IP) shows good FBPase inhibitory activity (IC50 = 0.22 μM), satisfying glucose-lowering effect in vivo (54% reduction in blood glucose at 25 mg/kg)[1].
FBPase-IN-1 (6 or 7 weeks, ICR mice, n = 6, male, 25 mg/kg, IP for 4 hours, once) reduces blood glucose levels by targeting FBPase and inhibiting the GNG process[1].

References:
[1]. Xu YX, Huang YY, Song RR, et al. Development of disulfide-derived fructose-1,6-bisphosphatase (FBPase) covalent inhibitors for the treatment of type 2 diabetes. Eur J Med Chem. 2020; 203: 112500.

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