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Anagliptin

Anagliptin
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Purity:100%
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Anagliptin

Catalog No. T7133Cas No. 739366-20-2
Anagliptin (SK-0403) is a potent inhibitor of DPP-4 (IC50 of 3.8 nM) used in the treatment of type 2 diabetes mellitus.
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Pack SizePriceAvailabilityQuantity
1 mg$39In Stock
5 mg$93In Stock
10 mg$155In Stock
25 mg$288In Stock
50 mg$493In Stock
100 mg$718In Stock
500 mg$1,470In Stock
1 mL x 10 mM (in DMSO)$98In Stock
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Product Introduction

Bioactivity
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.
Targets&IC50
DPP4:3.8 nM , DPP8:68 nM , DPP9:60 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].
AliasSK-0403
Chemical Properties
Molecular Weight383.45
FormulaC19H25N7O2
Cas No.739366-20-2
Storage & Solubility Information
StoragePowder: -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.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.6079 mL13.0395 mL26.0790 mL130.3951 mL
5 mM0.5216 mL2.6079 mL5.2158 mL26.0790 mL
10 mM0.2608 mL1.3040 mL2.6079 mL13.0395 mL
20 mM0.1304 mL0.6520 mL1.3040 mL6.5198 mL
50 mM0.0522 mL0.2608 mL0.5216 mL2.6079 mL
100 mM0.0261 mL0.1304 mL0.2608 mL1.3040 mL

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