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。
| 生物活性 | Cofrogliptin (HSK7653) (compound 2), a tetrahydropyran derivative, is a potent oraldipeptidylaminopeptidase4 (DPP-4)inhibitor with Long-acting antidiabetic efficacy. Cofrogliptin (compound 2) has a great potential for type 2 diabetes mellitus (T2DM)[1]. |
| IC50& Target | |
体外研究
(In Vitro) | Cofrogliptin (HSK7653) (compound 2) has the DPP-4 inhibitory activity with anIC50value of 4.18 nM[2].
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体内研究
(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[2].
| Animal Model: | ICR mice[2] | | Dosage: | 0.5 mg/kg, 2 mg/kg | | Administration: | IV: 0.5 mg/kg; PO: 2 mg/kg | | Result: | | | IV(dose: 0.5 mg/kg) | | | | PO(dose: 2 mg/kg) | | | | CI(mL/min/kg) | Vdss(L/kg) | t1/2(h) | | Cmax(ng/mL) | t1/2(h) | AUC0-t(ngoh/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 | [2] | 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[2] | | 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. |
| | Clinical Trial | | | 分子量 | | | Formula | | | CAS 号 | | | 运输条件 | Room temperature in continental US; may vary elsewhere. | | 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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