Molecular Formula | C16H15F6N5O.H3PO4 |
Molar Mass | 505.31 |
Melting Point | 202-204°C |
Boling Point | 529.9°C at 760 mmHg |
Flash Point | 274.3°C |
Solubility | Methanol (Slightly, Heated), Water (Sparingly, Sonicated) |
Vapor Presure | 2.59E-11mmHg at 25°C |
Appearance | Solid |
Color | White to Off-White |
Storage Condition | -20°C Freezer |
Physical and Chemical Properties |
|
Use | Sitagliptin and its intermediates (R & D) |
In vitro study | Sitagliptin phosphate exhibits a potent inhibitory effect on DPP-4 with IC 50 of 19 nM from Caco-2 cell extracts.Sitagliptin reduces in vitro migration of isolated splenic CD4 T-cells through a pathway involving cAMP/PKA/Rac1 activation.A recent study demonstrates that sitagliptin exerts a novel, direct action in order to stimulate GLP-1 secretion by the intestinal L cell through a DPP-4-independent, protein kinase A- and MEK-ERK1/2-dependent pathway. It therefore reduces the effect of autoimmunity on graft survival. |
In vivo study | In vivo, the ED 50 value of sitagliptin phosphate for inhibition of plasma DPP-4 activity is calculated to be 2.3 mg/kg 7 hour postdose and 30 mg/kg 24 hour postdose in freely fed Han-Wistar rats.The streptozotocin-induced type 1 diabetes mouse model exhibits elevated DPP-4 levels in the plasma that can be substantially inhibited in mice on an Sitagliptin phosphate diet. This is achieved by a positive effect on the regulation of hyperglycemia, potentially through prolongation of islet graft survival.The plasma clearance and volume of distribution of Sitagliptin phosphate are higher in rats (40-48 mL/min/kg, 7-9 L/kg) than in dogs (9 mL/min/kg, 3 L/kg); and its half-life is shorter in rats,2 hours compared with 4 hours in dogs. |