Evogliptin
Based on 1 publication(s) in Google Scholar
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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 1222102-29-5
- 分子式: C19H26F3N3O3
- 分子量:401.42
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
MedChemExpress(MCE)の使用を引用している文献 Evogliptin
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生物活性
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.
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Cell Line:H9 Th1 cells (pokeweed mitogen (PWM)-induced)
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Concentration:2.49 mM (1 µg/mL)
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Incubation Time:12 h
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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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male ICR mice (four-week-old; HFD/STZ mice model)[3].
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Dosage:100, 300 mg/kg
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Administration:In animal feedings; single daily for 10 weeks
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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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 1222102-29-5
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分子量 401.42
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分子式 C19H26F3N3O3
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SMILES
O=C1NCCN(C(C[C@H](N)CC2=CC(F)=C(F)C=C2F)=O)[C@@H]1COC(C)(C)C
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別名
DA-1229
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
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Journal Impact Factor
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Most Recent
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bioRxiv
Circulating biomarkers in serum from aortic valve stenosis patients predict sex-specific drug responses in valve myofibroblasts. [Abstract]2026 Jan 20:2026.01.16.700010. PMID: 41648356
純度とドキュメンテーション
参考文献
[1]. Yoon H, et al. Effects of the Antidiabetic Drugs Evogliptin and Sitagliptin on the Immune Function of CD26/DPP4 in Th1 Cells. Biomol Ther (Seoul). 2021 Mar 1;29(2):154-165. [Content Brief]
[3]. Kim TH, et al. Hepatic role in an early glucose-lowering effect by a novel dipeptidyl peptidase 4 inhibitor, evogliptin, in a rodent model of type 2 diabetes. Eur J Pharmacol. 2016 Jan 15;771:65-76. [Content Brief]
[4]. Tan X, et al. Evogliptin: a new dipeptidyl peptidase inhibitor for the treatment of type 2 diabetes. Expert Opin Pharmacother. 2016 Jun;17(9):1285-93. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)