1222102-29-5
1222102-29-5 structure
- Name: Evogliptin
- Chemical Name: (3R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-[(2-methylpropan-2-yl)oxymethyl]piperazin-2-one
- CAS Number: 1222102-29-5
- Molecular Formula: C19H26F3N3O3
- Molecular Weight: 401.42300
- Catalog: Signaling Pathways Autophagy Autophagy
- Create Date: 2016-09-14 23:05:34
- Modify Date: 2024-01-19 22:18:36
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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].
| Name | (3R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-[(2-methylpropan-2-yl)oxymethyl]piperazin-2-one |
|---|---|
| Synonyms |
Evogliptin [INN]
DA-1229 2-Piperazinone,4-((3R)-3-amino-1-oxo-4-(2,4,5-trifluorophenyl)butyl)-3-((1,1-dimethylethoxy)methyl)-,(3R) Evogliptin (R)-4-((R)-3-Amino-4-(2,4,5-trifluorophenyl)-butanoyl)-3-(t-butoxymethyl)-piperazin-2-one |
| Description | 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]. |
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| Related Catalog | |
| Target |
DPP4[1][2][3][4]. |
| In Vitro | 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]. 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. |
| In Vivo | 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]. 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. |
| Molecular Formula | C19H26F3N3O3 |
|---|---|
| Molecular Weight | 401.42300 |
| Exact Mass | 401.19300 |
| PSA | 88.15000 |
| LogP | 2.42000 |