伏格列波糖 T6723

Product Introduction
Bioactivity


英文名: Voglibose

描述: Voglibose (Glustat) 是一种 valiolamine 的衍生物，可抑制α-葡萄糖苷酶活性，可作用于高血糖症等。

体外活性: Voglibose能够抑制肠道内的α-葡萄糖苷酶，这些酶主要负责分解如麦芽糖和蔗糖等双糖，包括麦芽糖酶和蔗糖酶。Voglibose对蔗糖酶和麦芽糖酶的Ki值分别约为其对蔗糖和麦芽糖的Km值的10^6和10^5倍之小。[1]

体内活性: Voglibose (0.2 mg/kg) completely inhibits the insulin response to sucrose in rats. Voglibose (0.2 mg/kg) reduces the carbohydrate-induced increase in blood glucose in rats. Voglibose (0.2 mg/kg) reduces the carbohydrate-induced increase in blood glucose without causing sustained hypoglycemia in both normal and neonatal streptozotocin-induced diabetic rats. [2] Voglibose (0.001%) treatment increases GLP-1 secretion (Voglibose alone, 1.6-fold; Alogliptin plus Voglibose, 1.5-fold), while it decreases plasma glucose-dependent insulinotropic polypeptide (GIP) (Voglibose alone, 30%; Alogliptin plus voglibose, 29%) in prediabetic db/db mice after 3 weeks. Voglibose (0.001%) treatment decreases plasma DPP-4 activity by 15% in prediabetic db/db mice. Voglibose (0.001%) treatment increases plasma insulin by 1.8-fold and decreases plasma glucagon by 8% in prediabetic db/db mice. [3] Voglibose (0.001% and 0.005%) stimulates GLP-1 secretion in ob/ob mice, as evidenced by the 1.3- to 1.5-fold increase in plasma active plus inactive amidated GLP-1 levels. Voglibose (0.001% and 0.005%) decreases plasma DPP-4 activity unexpectedly by 40% to 51% in ob/ob mice, resulting from reduced plasma DPP-4 concentrations. Voglibose (0.001% and 0.005%) increases GLP-1 content by 1.5- to 1.6-fold and 1.4- to 1.6-fold in the lower intestine and colon, respectively, in ob/ob mice. [4]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 20.1 mg/mL (75 mM)
H2O : 26.7 mg/mL (100 mM)


关键字: inhibit | AO-128 | Inhibitor | Glucosidase | AO128 | Voglibose

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相关库: Drug Repurposing Compound Library | Glycometabolism Compound Library | FDA-Approved Kinase Inhibitor Library | FDA-Approved & Pharmacopeia Drug Library | Human Metabolite Library | Kinase Inhibitor Library | Inhibitor Library | Anti-Diabetic Compound Library | Anti-Obesity Compound Library | Target-Focused Phenotypic Screening Library

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