CAS NO: | 1222102-51-3 |
包装 | 价格(元) |
10mM (in 1mL DMSO) | 电议 |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
Cas No. | 1222102-51-3 |
别名 | DA-1229 tartrate |
Canonical SMILES | O=C1NCCN(C(C[C@H](N)CC2=CC(F)=C(F)C=C2F)=O)[C@@H]1COC(C)(C)C.O=C(O)[C@H](O)[C@@H](O)C(O)=O |
分子式 | C23H32F3N3O9 |
分子量 | 551.51 |
溶解度 | DMSO: 100 mg/mL (181.32 mM) |
储存条件 | Store at -20℃ |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | 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]. 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 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] [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. |