Alias

Sitagliptin Intermediate

Catalog Number

AP2406

CAS #

764667-65-4

Molecular Formula

C₁₆H₁₂F₆N₄O₂

Molecular Weight

406.28

Structural Formula

Product Introduction

CAS 764667-65-4

(2Z) -4-oxo-4- [3- (trifluoromethyl) -5,6-dihydro- [1,2,4] triazolo [4,3-a ] Pyrazine-7- (8H) -yl] -1- (2,4,5-trifluorophenyl) but-2-one, English name (2Z) -4-Oxo-4- [3- (trifluoromethyl ) -5,6-dihydro- [1,2,4]-triazolo [4,3-a] -pyrazine-7 (8H) -yl] -1- (2,4,5-trifluorophenyl) butan-2-one, American Chemical Abstracts Registration Number is cas 764667-65-4.

(2Z) -4-oxo-4- [3- (trifluoromethyl) -5,6-dihydro- [1,2,4] triazolo [4,3-a] pyrazine-7- (8H) -yl] -1- (2,4,5-trifluorophenyl) butan-2-one (CAS 764667-65-4) is a sitagliptin phosphate monohydrate intermediate. Sitagliptin phosphate monohydrate is a dipeptidyl peptidase-4 (DPP-4) inhibitor and controls blood glucose levels by protecting endogenous incretin and enhancing its effect. Glucose-dependent insulinotropic peptide (GIP) and glucagon-like peptide-1 (GLP-1) are incretins released against dietary intake. GLP-1 and GIP can increase insulin synthesis and release from islet β cells through intracellular signaling pathways. GLP-1 can also reduce glucagon secretion from islet α cells and reduce liver glucose production. However, both GLP-1 and GIP are rapidly metabolized by DPP-4, resulting in a loss of their insulinotropic effects. This medicine inhibits the degradation of incretin by DPP-4, so it can enhance the functions of GLP-1 and GIP, increase the release of insulin and reduce the glucagon level in the circulation (this effect is glucose-dependent). This drug selectively inhibits DPP-4 and has no inhibitory activity on DPP-8 or DPP-9. Can be used for the treatment of type 2 diabetes.