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1222102-51-3

1222102-51-3 structure
1222102-51-3 structure
  • Name: Evogliptin tartrate
  • Chemical Name: Evogliptin tartrate
  • CAS Number: 1222102-51-3
  • Molecular Formula: C23H32F3N3O9
  • Molecular Weight: 551.51
  • Catalog: Signaling Pathways Metabolic Enzyme/Protease Dipeptidyl Peptidase
  • Create Date: 2020-01-23 14:29:51
  • Modify Date: 2024-01-03 11:12:35
  • Evogliptin tartrate is a potent, orally bioavailable and selective dipeptidyl peptidase-4 (DPP-4) inhibitor, with antidiabetic activity. Evogliptin tartrate has potential for anti-atherosclerosis therapy that targets arterial inflammation[1].

Name Evogliptin tartrate
Description Evogliptin tartrate is a potent, orally bioavailable and selective dipeptidyl peptidase-4 (DPP-4) inhibitor, with antidiabetic activity. Evogliptin tartrate has potential for anti-atherosclerosis therapy that targets arterial inflammation[1].
Related Catalog
Target

DPP-4[1]

In Vitro 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)[1]. Evogliptin tartrate inhibits the TNF-α-mediated transcriptional activation of ICAM-1 and VCAM-1[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[1]. Cell Viability Assay[1] Cell Line: Endothelial cells Concentration: 0.1 μM, 0.3 μM, 1 μM, 3 μM Incubation Time: 12 hours Result: Inhibits TNF-α-mediated (10 ng/ml) expression of adhesion molecules.
In Vivo 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[1]. Evogliptin tartrate inhibits the formation of atherosclerotic lesions by reducing vasoinflammation and increases plaque stability[1]. Animal Model: ApoE−/− mice[1] Dosage: 37.5 mg/kg, 75 mg/kg, 150 mg/kg Administration: Oral administration; daily; for 12 weeks Result: Inhibit the development of atherosclerosis.
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.

Molecular Formula C23H32F3N3O9
Molecular Weight 551.51