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Postion:Product Catalog >Anagliptin
Anagliptin
  • Anagliptin

Anagliptin NEW

Price $39 $93 $155
Package 1mg 5mg 10mg
Min. Order:
Supply Ability: 10g
Update Time: 2024-11-14

Product Details

Product Name: Anagliptin CAS No.: 739366-20-2
Purity: 100% Supply Ability: 10g
Release date: 2024/11/14

Product Introduction

Bioactivity

名稱Anagliptin
描述Anagliptin (SK-0403) is a potent inhibitor of DPP-4 (IC50 of 3.8 nM) used in the treatment of type 2 diabetes mellitus.
動物實驗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].
體外活性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].
體內(nèi)活性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].
存儲條件Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度DMSO : 50 mg/mL (130.4 mM), Sonication is recommended.
關(guān)鍵字lipid‐lowering | smooth muscle cell | inhibit | DPP-4 | Dipeptidyl Peptidase | DPP | SK 0403 | DPP-8 | SMC | SK0403 | Anagliptin | atherosclerosis | Inhibitor
相關(guān)產(chǎn)品Sitagliptin | Sitagliptin phosphate monohydrate | Linagliptin | Vildagliptin | Alloxan monohydrate | 4'-Hydroxychalcone
相關(guān)庫高選擇性抑制劑庫 | 經(jīng)典已知活性庫 | 上市藥物庫 | ReFRAME 相關(guān)化合物庫 | 藥物功能重定位化合物庫 | 抑制劑庫 | NO PAINS 化合物庫 | 代謝化合物庫 | 臨床期小分子藥物庫 | 已知活性化合物庫

Company Profile Introduction

Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers. TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.

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