FBPase-IN-1,20362-54-3

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FBPase-IN-1

CAS No. : 20362-54-3

MCE 国际站：FBPase-IN-1

产品活性：FBPase-IN-1 是一种有效的 FBPase (Fructose-1,6-bisphosphatase) 抑制剂，IC₅₀ 为 0.22 μM，可用于二型糖尿病研究。FBPase-IN-1 可降低血糖水平，改善糖耐量。FBPase-IN-1 修饰 C128 位点，调控 FBPase 的 N125-S124-S123 变构通路，影响 FBPase 的催化活性。

研究领域：Metabolic Enzyme/Protease

作用靶点：FBPase

In Vitro: FBPase-IN-1 (compund 3a) (1.5625-200 μM, 48 hours) shows a low cytotoxicity with an IC₅₀ of 75.08 μM.
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.

In Vivo: 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).
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.

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