Cofrogliptin | MedChemExpress (MCE)
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MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。CofrogliptinCAS No. : 1844874-26-5MCE 国际站：Cofrogliptin产品活性：Cofrogliptin (HSK7653)
MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。
Cofrogliptin
CAS No. : 1844874-26-5
MCE 国际站：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.
Pharmacokinetic Parameters in ICR mice
| 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(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 |
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