Sitagliptin phosphate monohydrate Chemical Properties

Flash point:

274.3℃

storage temp. 

2-8°C

solubility 

≥23.8 mg/mL in DMSO; insoluble in EtOH; ≥30.6 mg/mL in H2O with ultrasonic

form 

solid

CAS DataBase Reference

654671-77-9(CAS DataBase Reference)

Safety Information

Risk Statements 

28-38-41-48-62-63

Safety Statements 

24/25-26-28-36/37/39

HS Code 

29335990

Sitagliptin phosphate monohydrate Usage And Synthesis

Chemical Properties

white crystalline

Uses

antimuscarinic

Uses

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

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.

target

DPP-4

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