Sitagliptin phosphate monohydrate

Chemical properties

white crystalline

The Uses of Sitagliptin phosphate monohydrate

antimuscarinic

The Uses of Sitagliptin phosphate monohydrate

Sitagliptin Phosphate Monohydrate is a dipeptidyl peptidase-IV (DPPIV) inhibitor.

What are the applications of Application

Sitagliptin phosphate monohydrate is a potent, active inhibitor of DPP-IV

Biological Activity

sitagliptin phosphate monohydrate is the phosphate salt of its active component, sitagliptin, with one molecule of water. sitagliptin is a potent inhibitor of dipeptidyl peptidase 4 (dpp-4), an enzyme catalyzing the cleavage of peptides with an n-terminal alanine or proline amino acid residue, that selectively inhibits dpp-4 with 50% inhibition concentration ic50 value of 18 nm and shows no affinity towards other ddp enzymes (such as ddp-8 and ddp-9). the inhibition of dpp4 by sitagliptin has been found to be mediated by increasing levels of two dpp-4 substrates, including glucagon-like peptide-1 (glp-1) and gastric inhibitory polypeptide (gip). sitagliptin is currently being investigated in the treatment of type ii diabetes.gallwitz b. review of sitagliptin phosphate: a novel treatment for type 2 diabetes. vasc health risk manag. 2007;3(2):203-10.

Chemical property

According to EMA reports, sitagliptin phosphate monohydrate doesn't exhibit a definite melting point as it decomposes at about 220°C. However, Stofella et al. reported a melting point of 120.29°C for the free base, 206.37°C for the monohydrate phosphate form and 214.92°C for the anhydrous phosphate form of sitagliptin.13 The thermal stability behaviour of the monohydrate and anhydrous forms of sitagliptin phosphate was similar, and both exhibited better thermal stability than the free base form.

Biological Activity

Sitagliptin phosphate monohydrate has been shown to lower HbA1c levels by about 0.7% points versus placebo. Sitagliptin phosphate is slightly less effective than metformin when used as a monotherapy and does not cause weight gain compared to sulfonylureas. Sitagliptin phosphate (MK-0431) reduces in vitro migration of isolated splenic CD4 T-cells through a cAMP/PKA/Rac1 activation pathway. The ED50 value of Sitagliptin phosphate for inhibition of plasma DPP-4 activity is 30 mg/kg 24 hours postdose in vivo.