| Description | Evogliptin tartrate has potential for anti-atherosclerosis therapy that targets arterial inflammation. Evogliptin tartrate is a potent, orally bioavailable and selective dipeptidyl peptidase-4 (DPP-4) inhibitor, with antidiabetic activity. |
| In vitro | Evogliptin tartrate inhibits the TNF-α-mediated transcriptional activation of ICAM-1 and VCAM-1. Evogliptin tartrate inhibits inflammatory responses via suppression of adhesion molecules induced by TNF-α. And TNF-α-mediated activation of NF-κB is ameliorated by evogliptin via the interaction of NF-κB with SIRT1.Evogliptin tartrate significantly inhibits the TNF-α-mediated induction of ICAM-1 and VCAM-1 expression in a concentration-dependent manner (IC50 = 0.30 and 0.25 μM, respectively). |
| In vivo | Evogliptin tartrate inhibits the formation of atherosclerotic lesions by reducing vasoinflammation and increases plaque stability.Evogliptin tartrate (37.5-150 mg/kg; p.o.; daily; for 12 weeks) reduces the high-fat diet-induced atherosclerotic plaque area in the ApoE?/? mouse model. |
| Synonyms | DA-1229 tartrate |
| molecular weight | 551.51 |
| Molecular formula | C23H32F3N3O9 |
| CAS | 1222102-51-3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| References | 1. Modulation of Sirt1/NF-κB interaction of evogliptin is attributed to inhibition of vascular inflammatory response leading to attenuation of atherosclerotic plaque formation. Biochem Pharmacol. 2019 Oct;168:452-464. |