Name | Saxagliptin monohydrate |
Synonyms | CS-1180 BMS477118 hydrate BMS 477118 hydrate Saxagliptin hydrate Saxagliptin monohydrate Saxagliptin hydrate Unii-9gb927lajw (1S,3S,5S)-2-[(2S)-2-Amino-2-(3-hydroxytricyclo[3.3.1.13,7]dec-1-yl)acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile hydrate (1s,3s,5s)-2-((2s)-2-amino-2-(3-hydroxytricyclo(3.3.1.13,7)dec-1-yl)acetyl)-2-azabicyclo(3.1.0)hexane-3-carbonitrile hydrate Saxagliptin hydrate (1S,3S,5S)-2-[(2S)-2-Amino-2-(3-hydroxytricyclo[3.3.1.1(3,7)]dec-1-yl)acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile hydrate |
CAS | 945667-22-1 |
EINECS | 641-082-3 |
InChI | InChI:1S/C18H25N3O2.H2O/c19-8-13-2-12-3-14(12)21(13)16(22)15(20)17-4-10-1-11(5-17)7-18(23,6-10)9-17;/h10-15,23H,1-7,9,20H2;1H2 |
Molecular Formula | C18H27N3O3 |
Molar Mass | 333.43 |
Melting Point | 106-108°C |
Solubility | DMSO (Slightly), Methanol (Sparingly) |
Appearance | Solid |
Color | White to Off-White |
Storage Condition | -20°C Freezer |
In vitro study | In vitro experiments, saxagliptin inhibited FBS, Sulin, IGF-1 induced ERK phosphorylation and cell proliferation in MSC and MC3T3E1 pre-osteoblasts. In the absence of growth factors, saxagliptin had no effect on ERK activation or cell proliferation. saxagliptin inhibited the expression of Runx2 and osteocalcin, the production of type I collagen, and mineralization in MSC and MC3T3 E1 Cells in the presence of FBS, increasing expression by PPAR-gamma. |
In vivo study | Saxagliptin has a direct beneficial effect on the arterial wall by increasing the utilization of NO and improving the antioxidant status in the animal model of type 2 diabetes. Saxagliptin by abrogating NAD(P)H oxidase-driven eNOS uncoupling and reducing COX-1 derived vasoconstrictor activity (activity of vasoconstrictors to down-regulate the expression of thromboxane prostaglandin receptors), reversal of vascular hypertrophic remodeling and improvement of NO availability in small vessels in db/db mice. Inhibition of Saxagliptin by DPP-4 also improved islet β-cell function and decreased postprandial glucagon concentration in both postprandial and fasting states. |