DPP-4inhibitor1(compound5)是有效的、长效的二肽基肽酶-4(DPP-4)的抑制剂，有治疗2型糖尿病的潜力，其KD值为0.177nM。
DPP-4 inhibitor 1 (compound 5) is a potent and long acting Dipeptidyl peptidase-4 (DPP-4) inhibitor for t treatment of T2DM, with a KD of 0.177 nM[1].
A single-dose oral administration of DPP-4 inhibitor 1 (compound 5) (3 mg/kg) inhibits >80% of DPP-4 activity for more than 7 days in diabetic mice[1].Administration of DPP-4 inhibitor 1 (compound 5) (3 and 10 mg/kg, p.o., qw for 8 weeks) causes significant reductions in fasting blood glucose (FBG) levels, and the average reduction during the entire treatment period is 24.7 and 33.1%, respectively. Chronic administration of DPP-4 inhibitor 1 (compound 5) (10 mg/kg/week) also significantly improves the glucose tolerance of the diabetic mice[1].|| Animal Model:|ICR mice[1].|Dosage:|0.3, 3, 10 mg/kg.|Administration:|Oral, once.|Result:|Resulted in a time- and dose-dependent inhibition of plasma DPP-4 activity.The active GLP-1 and insulin level were significantly increased compared with the vehicle control.|| Animal Model:|Genetic-type 2 diabetes animal models in db/db Mice[1].|Dosage:|3 and 10 mg/kg.|Administration:|Oral administration once a week, for 8 weeks.|Result:|Caused significant reductions in fasting blood glucose (FBG) levels.Improved the glucose tolerance of the diabetic mice significantly.
[1]. Li S, et al. Discovery of a Natural-Product-Derived Preclinical Candidate for Once-Weekly Treatment of Type 2 Diabetes. J Med Chem. 2019 Feb 1.
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