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Anagliptin

Catalog No. T7133 CAS 739366-20-2

Synonyms: SK-0403

Anagliptin (SK-0403) is a potent Inhibitor of DPP-4(IC50 of 3.8 nM), for the treatment of type 2 diabetes mellitus.

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Anagliptin, CAS 739366-20-2

Pack Size	Availability	Price/USD
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

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Purity: 100%

Biological Description

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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

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 95 mg/mL (247.75 mM), Sonification is recommended.

References and Literature

1. Ervinna N, et al. Anagliptin, a DPP-4 inhibitor, suppresses proliferation of vascular smooth muscles and monocyte inflammatory reaction and attenuates atherosclerosis in male apo E-deficient mice. Endocrinology. 2013 Mar;154(3):1260-70. 2. Yano W, et al. Mechanism of lipid-lowering action of the dipeptidyl peptidase-4 inhibitor, anagliptin, in low-density lipoprotein receptor-deficient mice. J Diabetes Investig. 2017 Mar;8(2):155-160.

Related compound libraries

This product is contained In the following compound libraries：

Highly Selective Inhibitor Library Inhibitor Library Drug Repurposing Compound Library Clinical Compound Library Approved Drug Library Bioactive Compounds Library Max Bioactive Compound Library HIF-1 Signaling Pathway Compound Library Ferroptosis Compound Library Ubiquitination Compound Library

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Keywords

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

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