Sitagliptin phosphate monohydrate

Biological Activity

Sitagliptin phosphate monohydrate is an oral antihyperglycemic (antidiabetic drug) of the dipeptidyl peptidase-4 (DPP-4) inhibitor class. Sitagliptin phosphate works to competitively inhibit the enzyme dipeptidyl peptidase 4 (DPP-4). This enzyme breaks down the incretins GLP-1 and GIP, gastrointestinal hormones released in response to a meal. Sitagliptin phosphate monohydrate has been shown to lower HbA1c level by about 0.7% points versus placebo. Sitagliptin phosphate is slightly less effective than metformin when used as a monotherapy and does not cause a weight gain compared to sulfonylureas. Sitagliptin phosphate (MK-0431) reduces in vitro migration of isolated splenic CD4 T-cells through a pathway involving cAMP/PKA/Rac1 activation. The ED50 value of Sitagliptin phosphate for inhibition of plasma DPP-4 activity is 30 mg/kg 24 hour postdose in vivo. Sitagliptin phosphate monohydrate is used for treatment of diabetes mellitus type 2.

Product Citations

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  Pharmacology. 2023;108(2):166-175.

  DPP4 Inhibitor Sitagliptin Reduces Inflammatory Responses and Mast Cell Activation in Allergic Rhinitis
  Sitagliptin phosphate monohydrate purchased from AbMole

Chemical Information

Molecular Weight	523.32
Formula	C16H15F6N5O.H3PO4.H2O
CAS Number	654671-77-9
Solubility (25°C)	Water 41 mg/mL DMSO 60 mg/mL
Storage	Powder          -20°C   3 years ;  4°C   2 years In solvent       -80°C   6 months ;  -20°C   1 month

References

[1] Herman GA, et al. J Clin Pharmacol. Pharmacokinetics and pharmacodynamic effects of the oral DPP-4 inhibitor sitagliptin in middle-aged obese subjects.