Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Anagliptin (SK-0403) is a potent Inhibitor of DPP-4(IC50 of 3.8 nM), for the treatment of type 2 diabetes mellitus.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 39.00 | |
5 mg | In stock | $ 93.00 | |
10 mg | In stock | $ 155.00 | |
25 mg | In stock | $ 288.00 | |
50 mg | In stock | $ 493.00 | |
100 mg | In stock | $ 718.00 | |
500 mg | In stock | $ 1,470.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 98.00 |
Description | Anagliptin (SK-0403) is a potent Inhibitor of DPP-4(IC50 of 3.8 nM), for the treatment of type 2 diabetes mellitus. |
Targets&IC50 | DPP8:68 nM , DPP9:60 nM, DPP4:3.8 nM |
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]. |
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]. |
Synonyms | SK-0403 |
Molecular Weight | 383.45 |
Formula | C19H25N7O2 |
CAS No. | 739366-20-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 95 mg/mL (247.75 mM), Sonication is recommended.
You can also refer to dose conversion for different animals. More
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Anagliptin 739366-20-2 Proteases/Proteasome Ubiquitination Proteasome DPP-4 lipid‐lowering smooth muscle cell inhibit Dipeptidyl Peptidase SK-0403 DPP SK 0403 DPP-8 SMC SK0403 atherosclerosis Inhibitor inhibitor