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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 |
| Related Dipeptidyl Peptidase Products |
|---|
| K579
K579 is a potent and orally active dipeptidyl peptidase IV inhibitor. |
| Retagliptin
Retagliptin (SP2086) is a selective, competitive and orally active dipeptidyl peptidase-4 (DPP-4) inhibitor. |
| Cofrogliptin
Cofrogliptin (HSK7653), a tetrahydropyran derivative, is a potent oral dipeptidyl aminopeptidase 4 (DPP-4) inhibitor with Long-acting antidiabetic efficacy. |
| Retagliptin phosphate
Retagliptin phosphate (SP2086 phosphate) is a selective, competitive and orally active dipeptidyl peptidase-4 (DPP-4) inhibitor. |
| Gly-Pro-pNA hydrochloride
Gly-Pro-pNA hydrochloride is a dipeptidyl peptidase inhibitor that inhibits dipeptidyl peptidase II, dipeptidyl peptidase IV and dipeptidyl peptidase IX. Gly-Pro-pNA hydrochloride is a chromogenic substrate that can be cleaved by the circulating enzyme, dipeptidyl peptidase IV (DPP IV). Gly-Pro-pNA can be used to screen for DPP IV inhibitors. |
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