2. Metabolic Enzyme/Protease Autophagy
  3. Dipeptidyl Peptidase Autophagy
  4. Evogliptin

Evogliptin (DA-1229) is an orally active DPP4 inhibitor with significant and sustained hypoglycaemic effects in mouse models. Evogliptin also inhibits the production of inflammatory and fibrotic signals in hepatocytes by inducing autophagy. Evogliptin can be used in studies of type 2 diabetes, osteoporosis, renal impairment and chronic liver inflammation.

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (Evogliptin tartrate) usually boasts enhanced water solubility and stability.

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Evogliptin

Evogliptin 構造式

CAS 番号 : 1222102-29-5

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Evogliptin 関連抗体

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製品説明

Evogliptin (DA-1229) is an orally active DPP4 inhibitor with significant and sustained hypoglycaemic effects in mouse models. Evogliptin also inhibits the production of inflammatory and fibrotic signals in hepatocytes by inducing autophagy. Evogliptin can be used in studies of type 2 diabetes, osteoporosis, renal impairment and chronic liver inflammation[1][2][3][4].

IC50 & Target
体外実験

Evogliptin (2.49 mM; 12 h) efficiently inhibits mDPP4 (membrane DPP4) enzymatic activity in PWM-induced H9 Th1 cells[1].
Evogliptin prevents inflammatory and fibrotic signaling through autophagy induction in primary hepatocytes of ATG7f/f-Cre+ mice[2].

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

Evogliptin 関連抗体

Cell Viability Assay[1]

Cell Line: H9 Th1 cells (pokeweed mitogen (PWM)-induced)
Concentration: 2.49 mM (1 µg/mL)
Incubation Time: 12 h
Result: Potently inhibited mDPP4 (membrane DPP4) activity in a dose-dependent manner but did not affect either the cytokine profile or cell viability in PWM-activated CD4+CD26+ H9 Th1 cells.
体内実験

Evogliptin (100, 300 mg/kg; in animal feedings; single daily for 10 weeks) exhibits antidiabetic effects on HFD/STZ mice and improves glucose intolerance and insulin resistance[3].

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

Animal Model: Male ICR mice (four-week-old; HFD/STZ mice model)[3].
Dosage: 100, 300 mg/kg
Administration: In animal feedings; single daily for 10 weeks
Result: Decreased the blood glucose level from the second weekand persisted through the 10-week treatment, when at 300 mg/kg.
Significantly reduced HbA1c level when dosage at 300 mg/kg.
Significantly decreased 6 h-fasted blood glucose levels in a dose-dependent manner.
臨床実験
分子量

401.42

分子式

C19H26F3N3O3
CAS 番号
SMILES

O=C1NCCN(C(C[C@H](N)CC2=CC(F)=C(F)C=C2F)=O)[C@@H]1COC(C)(C)C
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
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Evogliptin Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Evogliptin1222102-29-5DA-1229DA1229DA 1229Dipeptidyl PeptidaseAutophagyDPPtype 2 diabetesosteoporosisrenal impairmentchronic liver inflammationH9 Th1hepatocytesInhibitorinhibitorinhibit

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