产品
编 号：F747515
分子式：C18H19F5N4O3S
分子量：466.43
分子式：C18H19F5N4O3S
分子量：466.43
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
结构图
CAS No: 1844874-26-5
产品详情
生物活性：
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) .
体内研究：
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 miceIV(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%
Omarigliptin7.39±2.11.65±0.273.05±0.6798±1224.65±1.44095±55295.0±29
Cofrogliptin (compound 2)2.57±0.093.30±0.3325.6±9.6352±2029.9±3.27898±87362.2±6.9
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.
体外研究：
Cofrogliptin (HSK7653) (compound 2) has the DPP-4 inhibitory activity with an IC50 value of 4.18 nM.
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) .
体内研究：
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 miceIV(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%
Omarigliptin7.39±2.11.65±0.273.05±0.6798±1224.65±1.44095±55295.0±29
Cofrogliptin (compound 2)2.57±0.093.30±0.3325.6±9.6352±2029.9±3.27898±87362.2±6.9
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.
体外研究：
Cofrogliptin (HSK7653) (compound 2) has the DPP-4 inhibitory activity with an IC50 value of 4.18 nM.
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