Sitagliptin Sitagliptin Sitagliptin base
Product Name: Sitagliptin
Synonyms: Sitagliptin free base;(3R)-3-AMino-1-[3-(trifluoroMethyl)-5,6,7,8-tetrahydro-1,2,4-riazolo[4,3-a]pyrazin-7-yl]-4-(2,4,5-rifluorophenyl) butan-1-one;(R)-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;Sitagliptin (3R)-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-one;Sitagliptin base;(3R)-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-one;1,2,4-Triazolo(4,3-A)pyrazine, 7-((3R)-3-amino-1-oxo-4-(2,4,5-trifluorophenyl)butyl)-5,6,7,8-tetrahydor-3-(trifluoromethyl)-;Hsdb 7516
CAS: 486460-32-6
MF: C16H15F6N5O
MW: 407.32
EINECS: 690-730-1
Product Categories: API;Pharmaceutical intermediate;Heterocycles
Mol File: 486460-32-6.mol
Sitagliptin Chemical Properties
Melting point 114.1-115.7 °C
Boiling point 529.9±60.0 °C(Predicted)
density 1.61±0.1 g/cm3(Predicted)
pka 7.20±0.10(Predicted)
CAS DataBase Reference 486460-32-6(CAS DataBase Reference)
EPA Substance Registry System 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)-, (3R)- (486460-32-6)
Safety Information
Hazardous Substances Data 486460-32-6(Hazardous Substances Data)
Sitagliptin Usage And Synthesis
Description Sitagliptin, a dipeptidyl peptidase-4 (DPP-4) inhibitor, is a first-in-class oral drug launched for the treatment of type 2 diabetes. It acts by slowing the inactivation of incretins, which are endogenous peptides involved in the physiologic regulation of glucose homeostasis. Incretin hormones, including glucagonlike peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP), are released by the intestine throughout the day, and levels are increased in response to a meal. When blood glucose concentrations are normal or elevated,GLP-1 and GIP increase the synthesis and release of insulin from pancreatic b cells via intracellular signaling pathways involving cAMP. GLP-1 also lowers glucagon secretion from pancreatic αcells, which leads to reduced hepatic glucose production.
Originator Merck (US)
Uses Labeled Sitagliptin , intended for use as an internal standard for the quantification of Sitagliptin by GC- or LC-mass spectrometry.
Definition ChEBI: A triazolopyrazine that exhibits hypoglycemic activity.
Product Name: Sitagliptin
Synonyms: Sitagliptin free base;(3R)-3-AMino-1-[3-(trifluoroMethyl)-5,6,7,8-tetrahydro-1,2,4-riazolo[4,3-a]pyrazin-7-yl]-4-(2,4,5-rifluorophenyl) butan-1-one;(R)-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;Sitagliptin (3R)-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-one;Sitagliptin base;(3R)-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-one;1,2,4-Triazolo(4,3-A)pyrazine, 7-((3R)-3-amino-1-oxo-4-(2,4,5-trifluorophenyl)butyl)-5,6,7,8-tetrahydor-3-(trifluoromethyl)-;Hsdb 7516
CAS: 486460-32-6
MF: C16H15F6N5O
MW: 407.32
EINECS: 690-730-1
Product Categories: API;Pharmaceutical intermediate;Heterocycles
Mol File: 486460-32-6.mol
Sitagliptin Chemical Properties
Melting point 114.1-115.7 °C
Boiling point 529.9±60.0 °C(Predicted)
density 1.61±0.1 g/cm3(Predicted)
pka 7.20±0.10(Predicted)
CAS DataBase Reference 486460-32-6(CAS DataBase Reference)
EPA Substance Registry System 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)-, (3R)- (486460-32-6)
Safety Information
Hazardous Substances Data 486460-32-6(Hazardous Substances Data)
Sitagliptin Usage And Synthesis
Description Sitagliptin, a dipeptidyl peptidase-4 (DPP-4) inhibitor, is a first-in-class oral drug launched for the treatment of type 2 diabetes. It acts by slowing the inactivation of incretins, which are endogenous peptides involved in the physiologic regulation of glucose homeostasis. Incretin hormones, including glucagonlike peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP), are released by the intestine throughout the day, and levels are increased in response to a meal. When blood glucose concentrations are normal or elevated,GLP-1 and GIP increase the synthesis and release of insulin from pancreatic b cells via intracellular signaling pathways involving cAMP. GLP-1 also lowers glucagon secretion from pancreatic αcells, which leads to reduced hepatic glucose production.
Originator Merck (US)
Uses Labeled Sitagliptin , intended for use as an internal standard for the quantification of Sitagliptin by GC- or LC-mass spectrometry.
Definition ChEBI: A triazolopyrazine that exhibits hypoglycemic activity.
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