Anagliptin is an orally active, potent and selective dipeptidyl peptidase 4 (DPP-IV; DPP4) inhibitor (DPP4/8/9 IC50 = 3.8/68/60 nM). When administered in vivo (0.3% w/w in diet), anagliptin shows anti-atherosclerotic efficay in apoE-deficient mice and ameliorates diabetes in mice with haploinsufficiency of glucokinase on a high-fat diet.
Orally active, potent and selective dipeptidyl peptidase 4 (DPP-IV; DPP4) inhibitor with anti-atherosclerotic and anti-diabetic efficacy in vivo.
In the course of our program for discovery of novel DPP-IV inhibitors, a series of pyrazolo[1,5-a]pyrimidines were found to be novel DPP-IV inhibitors. We identified N-[2-({2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl}amino)-2-methylpropyl]-2-methylpyrazolo[1,5-a]pyrimidine-6-carboxamide hydrochloride (4a) and described its pharmacological profiles.
Metabolism: clinical and experimental, 62(7), 939-951 (2013-06-26)
Type 2 diabetes is a chronic metabolic disorder characterized by hyperglycemia with insulin resistance and impaired insulin secretion. DPP-4 inhibitors have attracted attention as a new class of anti-diabetic agents for the treatment of type 2 diabetes. We investigated the
Dipeptyl peptidase-4 (DPP-4) inhibitors modulate the progression of atherosclerosis. To gain insights into their mechanism of action, 9-wk-old male apolipoprotein E (apoE)-deficient mice were fed a DPP-4 inhibitor, anagliptin-containing diet. The effects of anagliptin were investigated in, a monocyte cell
