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Cofrogliptin

CAS No. : 1844874-26-5

MCE 站：Cofrogliptin

产品活性：Cofrogliptin (HSK7653) (compound 2)，一种四氢吡喃衍生物，是一种有效的口服 DPP-4 抑制剂，具有长效降糖作用。Cofrogliptin (compound 2) 在2型糖尿病 (T2DM) 应用中具有很大的潜力。

研究领域：Metabolic Enzyme/Protease

作用靶点：Dipeptidyl Peptidase

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

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 levelat 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.

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