| Name | Saxagliptin hydrate |
| Description | Saxagliptin hydrate (Onglyza hydrate) is a selective and reversible DPP4 inhibitor (IC50: 26 nM; Ki: 1.3 nM). |
| Cell Research | 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) |
| 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]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 70 mg/mL (209.94 mM), Sonication is recommended.
H2O : 1 mg/mL (3 mM)
Ethanol : 61 mg/mL (182.9 mM)
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| Keywords | Saxagliptin hydrate | DPP | glucagon-like | c-myc | BMS-477118 | glucagon | β-catenin | BMS 477118 | Saxagliptin | BMS477118 | insulin | proliferation | Onglyza Hydrate | p-AKT | Inhibitor | peptide-1 | BMS-477118 Hydrate | diabetes | Dipeptidyl Peptidase | DPP-4 | Saxagliptin Hydrate | BMS477118 Hydrate | inhibit | BMS 477118 Hydrate |
| Inhibitors Related | Sitagliptin | Teneligliptin hydrobromide | Sitagliptin phosphate monohydrate | Anagliptin | TCH-165 | Racecadotril | Linagliptin | Aprotinin | Vildagliptin | Alloxan monohydrate | 4'-Hydroxychalcone | Bortezomib |
| Related Compound Libraries | Highly Selective Inhibitor Library | Bioactive Compound Library | Approved Drug Library | HIF-1 Signaling Pathway Compound Library | EMA Approved Drug Library | Drug Repurposing Compound Library | Inhibitor Library | FDA-Approved Drug Library | Orally Active Compound Library | Bioactive Compounds Library Max |
United States
