1. Metabolic Enzyme/Protease
  2. Dipeptidyl Peptidase
  3. Evogliptin tartrate

Evogliptin tartrate (Synonyms: DA-1229 tartrate)

Cat. No.: HY-117985B
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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.

For research use only. We do not sell to patients.

Evogliptin tartrate Chemical Structure

Evogliptin tartrate Chemical Structure

CAS No. : 1222102-51-3

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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].

IC50 & 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.
Clinical Trial
Molecular Weight

551.51

Formula

C₂₃H₃₂F₃N₃O₉

CAS No.

1222102-51-3

SMILES

O=C1NCCN(C(C[[email protected]](N)CC2=CC(F)=C(F)C=C2F)=O)[[email protected]@H]1COC(C)(C)C.O=C(O)[[email protected]](O)[[email protected]@H](O)C(O)=O

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

EvogliptinDA-1229DA1229DA 1229Dipeptidyl PeptidaseDPPDPP-4antidiabeticatherosclerosisInhibitorinhibitorinhibit

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Evogliptin tartrate
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