Cofrogliptin

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) In Vitro Cofrogliptin (HSK7653) (compound 2) has the DPP-4 inhibitory activity with an IC 50 value of 4.18 nM. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo 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. Pharmacokinetic Parameters in ICR miceIV(dose: 0.5 mg/kg) PO(dose: 2 mg/kg) CI(mL/min/kg) V dss (L/kg) t 1/2 (h) C max (ng/mL) t 1/2 (h) AUC 0-t (ng•h/mL) F% Omarigliptin 7.39±2.1 1.65±0.27 3.05±0.6 798±122 4.65±1.4 4095±552 95.0±29 Cofrogliptin (compound 2) 2.57±0.09 3.30±0.33 25.6±9.6 352±20 29.9±3.2 7898±873 62.2±6.9 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: ob/ob miceDosage: 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 monkeysDosage: 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. Form:Solid IC50& Target:DPP-4

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