Cofrogliptin

Research use only, not for human use.

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).

Cofrogliptin (HSK7653) (compound 2), a tetrahydropyran derivative, is a potent oral dipeptidyl aminopeptidase 4 (DPP-4) inhibitor with Long-acting antidiabetic efficacy. Cofrogliptin (compound 2) has a great potential for type 2 diabetes mellitus (T2DM) .

Cofrogliptin (HSK7653) (compound 2) has the DPP-4 inhibitory activity with an IC50 value of 4.18 nM.

Cofrogliptin (HSK7653) (compound 2) (IV: 0.5 mg/kg; PO: 2 mg/kg) exhibits extremely long half-lives and low rate of reduction of drug concentration after orally administration.Cofrogliptin (compound 2) (Single, orally, 3 mg/kg, 10 mg/kg, 30 mg/kg) increases of half-lives, has high oral exposure, low i.v. clearance and hepatic microsomal clearance after intravenous dosing. Cofrogliptin (compound 2) (Single, orally, 10 mg/kg) exhibits longe inhibition time of DPP-4 and decreases HbA1c level at the doses of 3 and 10 mg/kg in ob/ob mice. Cofrogliptin (compound 2) (Single, orally, 10 mg/kg) also has a great potential of biweekly regimen for T2DM as indicated in rhesus monkeys.Animal Model:ob/ob mice Dosage:3 mg/kg, 10 mg/kg, 30 mg/kg Administration: Single, orally, 3 mg/kg, 10 mg/kg, 30 mg/kg Result:Exhibited strong inhibition capability of plasma DPP-4 in a dose dependent manner. Animal Model:rhesus monkeys Dosage:10 mg/kg Administration:Single, orally, 10 mg/kg Result: Possessed the capability of plasma DPP-4 inhibition over 80% for at least 12 days.Remained the plasma DPP-4 inhibition rates of 76.16% and 43.41%, respectively at the end of second week and third week after administration.

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Metabolic Enzyme/Protease

DPP

DPP-4

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1844874-26-5

466.43

C18H19F5N4O3S

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (214.39 mM; Ultrasonic )

C(F)(F)(F)[C@@H]1[C@@H](C[C@H](N)[C@H](O1)C2=C(F)C=CC(F)=C2)N3CC=4C(C3)=NN(S(C)(=O)=O)C4

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(-20℃)

With Ice Pack

≥ 2 years