Saxagliptin hydrate

For research use only.

Catalog No.S4697 Synonyms: BMS-477118 hydrate, Onglyza hydrate, BMS 477118 hydrate, BMS477118 hydrate

Saxagliptin hydrate Chemical Structure

Molecular Weight(MW): 333.43

Saxagliptin H2O is a selective and reversible DPP4 inhibitor with IC50 of 26 nM.

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Biological Activity

Description Saxagliptin H2O is a selective and reversible DPP4 inhibitor with IC50 of 26 nM.
Targets
DPP-4 [1]
()
In vitro

In vitro, saxagliptin inhibits FBS-, insulin- and IGF1-induced ERK phosphorylation and cell proliferation, in both MSC and MC3T3E1 preosteoblasts. In the absence of growth factors, saxagliptin has no effect on ERK activation or cell proliferation. In both MSC and MC3T3E1 cells, saxagliptin in the presence of FBS inhibits Runx2 and osteocalcin expression, type-1 collagen production and mineralization, while increasing PPAR-gamma expression[4].

In vivo Saxagliptin exerts direct beneficial effects on the arterial wall in an animal model of type 2 diabetes by increasing NO availability and improving antioxidant status. Saxagliptin reverses vascular hypertrophic remodeling and ameliorates NO availability in small arteries from db/db mice through the abrogation of NAD(P)H oxidase-driven eNOS uncoupling and by reducing the action of cyclooxygenase-1-derived vasoconstrictors downregulating the expression of thromboxane-prostanoid receptors[2]. DPP-4 inhibition with saxagliptin also improves pancreatic β-cell function in postprandial and fasting states, and decreases postprandial glucagon concentration[3].

Protocol

Cell Research:

[4]

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  • Cell lines: Marrow stromal cells(MSC); MC3T3E1 osteoblast-like cells
  • Concentrations: 1.5 or 15 μM
  • Incubation Time: 24 h or 1 h
  • Method:

    Sub-confluent cells are serum-starved overnight and then incubated with 1.5 or 15 μM saxagliptin and/or FBS (1%), insulin (5 ng/mL) or IGF1 (10-8 M) for 24 h (effects on cell proliferation) or 1 h (effects on signal transduction mechanisms).


    (Only for Reference)
Animal Research:

[2]

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  • Animal Models: adult mice C57BLKS/J; db/db mice
  • Dosages: 0.1 mg/kg
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 66 mg/mL (197.94 mM)
Ethanol 66 mg/mL (197.94 mM)
Water 1 mg/mL (2.99 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 333.43
Formula

C18H25N3O2.H2O

CAS No. 945667-22-1
Storage powder
in solvent
Synonyms BMS-477118 hydrate, Onglyza hydrate, BMS 477118 hydrate, BMS477118 hydrate
Smiles O.NC(C(=O)N1C(CC2CC12)C#N)[C]34CC5[CH2]C(C[C](O)(C5)C3)C4

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID