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.
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
| 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 |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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