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.
Product information
CAS Number: 1222102-51-3
Molecular Weight: 551.51
Formula: C23H32F3N3O9
Chemical Name: (2R,3R)-2,3-dihydroxybutanedioic acid; (3R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-[(tert-butoxy)methyl]piperazin-2-one
Smiles: CC(C)(C)OC[C@@H]1C(=O)NCCN1C(=O)C[C@H](N)CC1=CC(F)=C(F)C=C1F.OC(=O)[C@H](O)[C@@H](O)C(O)=O
InChiKey: RBBXDAJRSNHIJZ-DLDKMZOSSA-N
InChi: InChI=1S/C19H26F3N3O3.C4H6O6/c1-19(2,3)28-10-16-18(27)24-4-5-25(16)17(26)8-12(23)6-11-7-14(21)15(22)9-13(11)20;5-1(3(7)8)2(6)4(9)10/h7,9,12,16H,4-6,8,10,23H2,1-3H3,(H,24,27);1-2,5-6H,(H,7,8)(H,9,10)/t12-,16-;1-,2-/m11/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 100 mg/mL (181.32 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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). 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.
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. Evogliptin tartrate inhibits the formation of atherosclerotic lesions by reducing vasoinflammation and increases plaque stability.
Products are for research use only. Not for human use.
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