Name | DPP-4 inhibitor 1 |
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Description | 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]. |
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Related Catalog | |
Target |
KD: 0.177 nM (DPP-4)[1]. |
In Vivo | 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. |
References |
Molecular Formula | C21H15F3N2O2 |
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Molecular Weight | 384.35 |