Evogliptin tartrate (C09-1130-450)

Evogliptin (DA-1229) tartrate is an orally active DPP4 inhibitor with significant and sustained hypoglycaemic effects in mouse models. Evogliptin tartrate also inhibits the production of inflammatory and fibrotic signals in hepatocytes by inducing autophagy . Evogliptin tartrate can be used in studies of type 2 diabetes, osteoporosis, renal impairment and chronic liver inflammationIn VitroEvogliptin tartrate (2.49 mM; 12 h) efficiently inhibits mDPP4 (membrane DPP4) enzymatic activity in PWM-induced H9 Th1 cells. Evogliptin tartrate prevents inflammatory and fibrotic signaling through autophagy induction in primary hepatocytes of ATG7 f/f -Cre + mice. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell 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 VivoEvogliptin tartrate (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. 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). 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.Form:SolidIC50& Target:DPP-4. Specifications and Purity: 99%. Molecular Formula: C19H26F3N3O3•(C4H6O6). Molecular Weight: 401.4215009. PubChem CID: 135395528. Isomeric SMILES: CC(C)(C)OC[C@@H]1C(=O)NCCN1C(=O)C[C@@H](CC2=CC(=C(C=C2F)F)F)N.[C@@H]([C@H](C(=O)O)O)(C(=O)O)O.