1. Metabolic Enzyme/Protease
  2. Dipeptidyl Peptidase
  3. Cofrogliptin

Cofrogliptin (Synonyms: HSK7653)

Cat. No.: HY-147257
Handling Instructions

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) .

For research use only. We do not sell to patients.

Cofrogliptin Chemical Structure

Cofrogliptin Chemical Structure

CAS No. : 1844874-26-5

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Description

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) [1].

IC50 & Target

IC50: 4.18 nM (DPP-4) [2]

In Vitro

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

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[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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(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
Animal Model: ob/ob mice[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.
Molecular Weight

466.43

Formula

C18H19F5N4O3S

CAS No.
SMILES

FC(F)([[email protected]@H](O[[email protected]]1([H])C(C=C2F)=C(C=C2)F)[[email protected]@](N(CC3=N4)CC3=CN4[S](C)(=O)=O)([H])C[[email protected]@H]1N)F

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Cofrogliptin
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