| Name | Anagliptin |
| Description | Anagliptin (SK-0403) is a potent inhibitor of DPP-4 (IC50 of 3.8 nM) used in the treatment of type 2 diabetes mellitus. |
| Animal Research | Male low-density lipoprotein receptor-deficient mice were administered 0.3% anagliptin in their diet.?Plasma lipid levels were assayed and lipoprotein profile was analyzed using high-performance liquid chromatography.?Hepatic gene expression was examined by deoxyribonucleic acid microarray and quantitative polymerase chain reaction analyses[2]. |
| In vitro | Soluble DPP-4 augmented cultured SMC proliferation, and anagliptin suppressed the proliferation by inhibiting ERK phosphorylation.?In THP-1 cells, anagliptin reduced lipopolysaccharide-induced TNF-α production with inhibiting ERK phosphorylation and nuclear translocation of nuclear factor-κB.?Quantitative analysis also showed that anagliptin reduced the area of atherosclerotic lesion in apoE-deficient mice[1]. |
| In vivo | Treatment with anagliptin for 16 wk significantly reduced accumulation of monocytes and macrophages in the vascular wall, SMC content in plaque areas, and oil red O-stained area around the aortic valve without affecting glucose tolerance or body weight.?Serum DPP-4 concentrations were significantly higher in apoE-deficient mice than control mice, and the levels increased with aging, suggesting the involvement of DPP-4 in the progression of atherosclerosis[1]. Anagliptin treatment significantly decreased the plasma total cholesterol (14% reduction, P < 0.01) and triglyceride levels (27% reduction, P < 0.01). Both low-density lipoprotein cholesterol and very low-density lipoprotein cholesterol were also decreased significantly by anagliptin treatment. Sterol regulatory element-binding protein-2 messenger ribonucleic acid expression level was significantly decreased at night in anagliptin-treated mice (15% reduction, P < 0.05). Anagliptin significantly suppressed sterol regulatory element-binding protein activity in HepG2 cells (21% decrease, P < 0.001)[2]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 50 mg/mL (130.4 mM), Sonication is recommended.
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| Keywords | lipid‐lowering | smooth muscle cell | inhibit | DPP-4 | Dipeptidyl Peptidase | DPP | SK 0403 | DPP-8 | SMC | SK0403 | Anagliptin | atherosclerosis | Inhibitor |
| Inhibitors Related | Sitagliptin | Sitagliptin phosphate monohydrate | Linagliptin | Vildagliptin | Alloxan monohydrate | 4'-Hydroxychalcone |
| Related Compound Libraries | Highly Selective Inhibitor Library | Bioactive Compound Library | Approved Drug Library | ReFRAME Related Library | Drug Repurposing Compound Library | Inhibitor Library | NO PAINS Compound Library | Metabolism Compound Library | Clinical Compound Library | Bioactive Compounds Library Max |
United States
