Orally active, potent and selective dipeptidyl peptidase IV (DPP-IV; DPP4) inhibitor that improves glucose tolerance in vivo.
Sitagliptin is an orally active, potent and selective dipeptidyl peptidase IV (DPP4; DPP-IV) inhibitor (IC50 = 18 nM) with excellent selectivity over other proline-selective peptidases (IC50 = 48 μM/DPP8, >100 μM/DPP9 & QPP). Sitagliptin improves glucose tolerance in lean mice (23% and 55% reduction of blood glucose post 5 g dextrose/kg with 0.1 or 3 mg Sitagliptin/kg p.o. 60 min prior to dextrose challenge) and in DIO mice (68% and 90% reduction of blood glucose post 2 g dextrose/kg with 0.3 or 3 mg Sitagliptin/kg p.o.) as a result of DPP-IV inhibition and upregulated GLP-1 level in blood in vivo.
We previously tested two angiotensin-converting enzyme (ACE) inhibitors and two dipeptidyl peptidase-4 (DPP-4) inhibitors for dual enzyme inhibitory effect. Only two DPP-4 inhibitors, linagliptin and sitagliptin, were able to inhibit ACE. In the present study, we investigated if other inhibitors
Journal of diabetes and metabolic disorders, 20(1), 551-560 (2021-07-06)
Emerging evidence suggests that mesenchymal stem cells (MSCs) have many anti-inflammatory and regenerative properties, which makes it a suitable candidate for the treatment of many diseases including metabolic syndrome (MetS). However, a major difficulty with stem cell therapy is to
Frontiers in oncology, 11, 679816-679816 (2021-06-15)
Cancer has been as one of common comorbidities of diabetes. Long-term antidiabetic treatment may potentially exert uncertain impacts on diabetic patients with cancer including breast cancer (BC). Dipeptidyl peptidase-4 inhibitors (DPP-4i) are currently recommended by the AACE as first-line hypoglycemic
Iranian journal of basic medical sciences, 24(4), 451-459 (2021-06-08)
Fatty liver disease (FLD) is a disorder related to accumulation of excess fat within the hepatocytes. In this study, the effects of Berberine, a natural compound, and Sitagliptin as a DPP-4 inhibitor, were observed in a rat model of FLD.
Journal of medicinal chemistry, 48(1), 141-151 (2005-01-07)
A novel series of beta-amino amides incorporating fused heterocycles, i.e., triazolopiperazines, were synthesized and evaluated as inhibitors of dipeptidyl peptidase IV (DPP-IV) for the treatment of type 2 diabetes. (2R)-4-Oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine (1) is a potent, orally active DPP-IV inhibitor (IC(50) =
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