Basic information Safety Supplier Related

rac-Sitagliptin

Basic information Safety Supplier Related

rac-Sitagliptin Basic information

Product Name:
rac-Sitagliptin
Synonyms:
  • 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
  • 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
  • rac-SitagliptinSee: S491000
  • 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
  • 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
  • 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
  • rac-Sitagliptin
  • 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)-
CAS:
823817-56-7
MF:
C16H15F6N5O
MW:
407.31
Product Categories:
  • All Inhibitors
  • Inhibitors
  • Intermediates & Fine Chemicals
  • Pharmaceuticals
  • Bases & Related Reagents
  • Nucleotides
Mol File:
823817-56-7.mol
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rac-Sitagliptin Chemical Properties

Boiling point:
529.9±60.0 °C(Predicted)
Density 
1.61±0.1 g/cm3(Predicted)
storage temp. 
Refrigerator
solubility 
DMSO, Ethyl Acetate, Methanol
pka
7.20±0.10(Predicted)
form 
Oil
color 
Yellow to Light Brown
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rac-Sitagliptin Usage And Synthesis

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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