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 |
|---|
| Sitagliptin phosphate monohydrate
Sitagliptin phosphate (MK-0431) is a potent inhibitor of dipeptidyl peptidase-4 (DPP-4) with IC50 of 19 nM. |
| Trelagliptin
Trelagliptin (SYR-472) is a novel once-weekly oral DPP-4 inhibitor for type 2 diabetes. |
| Alogliptin
Alogliptin is a potent, selective inhibitor of DPP-4 with IC50 of <10 nM, exhibits greater than 10,000-fold selectivity over DPP-8 and DPP-9. |
| Linagliptin
Linagliptin is a highly potent, selective DPP-4 inhibitor with IC50 of 1 nM. |
| Vildagliptin
Vildagliptin (LAF237) is a potent, stable, selective dipeptidyl peptidase IV (DPP-IV) inhibitor with an IC50 of 3.5 nM in human Caco-2 cells. Vildagliptin possesses excellent oral bioavailability and potent antihyperglycemic activity. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
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