All AbMole products are for research use only, cannot be used for human consumption.
Trelagliptin(SYR-472) succinate is selective over other related DPP enzymes, P450 enzymes and hERG channel. Trelagliptin(SYR-472) succinate exhibits approximately 4- and 12-fold more potent inhibition against human dipeptidyl peptidase-4 than alogliptin and sitagliptin, respectively, and >10,000-fold selectivity over related proteases including dipeptidyl peptidase-8 and dipeptidyl peptidase-9. Kinetic analysis reveals reversible, competitive and slow-binding inhibition of dipeptidyl peptidase-4 by trelagliptin (t1/2 for dissociation ≈ 30 minutes). X-ray diffraction data indicates a non-covalent interaction between dipeptidyl peptidase and trelagliptin.
Currently, all available DPP-4 inhibitors are dosed once-daily. Phase III clinical studies with trelagliptin in Japan to evaluate its safety and efficacy in a once-weekly oral treatment regimen.
Pharmacology. 2023;108(2):166-175.
DPP4 Inhibitor Sitagliptin Reduces Inflammatory Responses and Mast Cell Activation in Allergic Rhinitis
Trelagliptin succinate purchased from AbMole
| Molecular Weight | 475.47 |
| Formula | C18H20FN5O2.C4H6O4 |
| CAS Number | 1029877-94-8 |
| Solubility (25°C) | DMSO 90 mg/mL Water 90 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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Products are for research use only. Not for human use. We do not sell to patients.
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