Cofrogliptin (HSK7653) is an orally available dipeptidyl peptidase-4 (DPP-4) inhibitor with hypoglycemic effects, which can be used to study type 2 diabetes (T2D).

DPP4:4.2 nM

Evaluate the DPP-4 inhibitory activities of Cofrogliptin, Cofrogliptin exhibited a much better in vitro activity, which significantly enhanced the potency IC50 = 4.2 nM. [1]

In vehicle group, mice were intragastrically given 1% hypromellose at a volume of 20 mL/kg. In treatment groups, mice were intragastrically administrated either omarigliptin at 30 mg/kg or varying doses of Cofrogliptin. Cofrogliptin inhibitory activity on plasma DPP-4 was assayed ex vivo in ob/ob mice. After a single dose, Cofrogliptin exhibited a much stronger inhibition capability of plasma DPP-4 than omarigliptin in a dose dependent manner.
Monkeys were intragastrically administrated either vehicle or Cofrogliptin (10 mg/kg) at a volume of 5 mL/kg. The ex vivo plasma DPP-4 inhibition was also assayed for Cofrogliptin in rhesus monkeys. After a single dose of 10 mg/kg, Cofrogliptin possessed the capability of plasma DPP-4 inhibition over 80% for at least 12 days. [1]