| Identification | Back Directory | [Name]
rac-Sitagliptin | [CAS]
823817-56-7 | [Synonyms]
rac-Sitagliptin
rac-SitagliptinSee: S491000
7-[3-Amino-1-oxo-4-(2,4,5-trifluorophenyl)butyl]-5,6,7,8-tetrahydro-3-(trifluoromethyl)-1,2,4-triazolo[4,3-a]pyrazine
7-[1-Oxo-3-amino-4-(2,4,5-trifluorophenyl)butyl]-3-(trifluoromethyl)-5,6,7,8-tetrahydro-1,2,4-triazolo[4,3-a]pyrazine
7-[3-Amino-1-oxo-4-(2,4,5-trifluorophenyl)butyl]-5,6,7,8-tetrahydro-3-(trifluoromethyl)-1,2,4-triazolo[4,3-α]pyrazine
3-AMino-1-[3-(trifluoroMethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-(2,4,5-trifluorophenyl)-1-butanone
3-aMino-1-(3-(trifluoroMethyl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-4-(2,4,5-trifluorophenyl)butan-1-one
1-Butanone,3-amino-1-[5,6-dihydro-3-(trifluoromethyl)-1,2,4-triazolo[4,3-a]pyrazin-7(8H)-yl]-4-(2,4,5-trifluorophenyl)-
3-Amino-1- [3- (trifluoromethyl) -5,6,7,8-tetrahydro-1,2,4-triazolo [4,3-a] pyrazin-7-yl] -4- (2,4,5-trifluorophenyl) butan-1 | [Molecular Formula]
C16H15F6N5O | [MOL File]
823817-56-7.mol | [Molecular Weight]
407.316 |
| Chemical Properties | Back Directory | [Appearance]
Light Brown Syrup | [Boiling point ]
529.9±60.0 °C(Predicted) | [density ]
1.61±0.1 g/cm3(Predicted) | [storage temp. ]
Refrigerator | [solubility ]
DMSO, Ethyl Acetate, Methanol | [form ]
Oil | [pka]
7.20±0.10(Predicted) | [color ]
Yellow to Light Brown |
| Hazard Information | Back Directory | [Chemical Properties]
Light Brown Syrup | [Uses]
A trizolopyrazine dipeptidyl peptidase IV inhibitor. It has recently been approved for the therapy of type II diabetes. | [in vivo]
In vivo, the ED50 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[1].?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[4].?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[5]. |
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