CAS 945667-22-1 | Saxagliptin

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

In vitro studies

In vitro, saxagliptin inhibited FBS, insulin, and IGF-1-induced ERK phosphorylation and cell proliferation in MSCs and MC3T3E1 preosteoblasts. In the absence of growth factors, saxagliptin had no effect on ERK activation of Chemicalbook or cell proliferation. In MSC and MC3T3E1 cells, in the presence of FBS, saxagliptin inhibited Runx2 and osteocalcin expression, collagen I production, and mineralization, and increased PPAR-gamma expression.

In vivo studies

Saxagliptin has a direct beneficial effect on the arterial wall by increasing NO utilization and improving antioxidant status in animal models of type 2 diabetes. Saxagliptin reverses vascular hypertrophy by abrogating NAD(P)H oxidase-driven uncoupling of eNOS and reducing COX-1-derived vasoconstrictor activity Chemicalbook (activity of vasoconstrictors to downregulate the expression of thromboxane prostaglandin receptors) plastics and improves NO availability in small blood vessels in db/db mice. Saxagliptin inhibits DPP-4 and can also improve islet β-cell function and reduce postprandial glucagon concentrations in postprandial and fasted states.

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