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 |
| 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.
| Related Dipeptidyl Peptidase Products |
|---|
| HAEGT
HAEGT is the first N-terminal 1-5 residues of glucagon like peptide-1 (GLP-1) peptide, and the sequence is His-Ala-Glu-Gly-Thr. |
| Diprotin B
Diprotin B is a dipeptidyl aminopeptidase IV (DPP IV) inhibitor. |
| Azaleatin
Azaleatin is an O-methylated flavonol isolated from Rhododendron species. Azaleatin is a dipeptidyl peptidase-IV inhibitor. Azaleatin can be used for the research of type-2 diabetes and obesity. |
| Sitagliptin fenilalanil hydrochloride
Sitagliptin fenilalanil hydrochloride is a dipeptidyl aminopeptidase 4 (DPP-4) inhibitor. |
| Lys-Ala-pNA
Lys-Ala-pNA is hydrolytic substrate the of dipeptidyl peptidase (DPP) II with Km of 0.42 mM. |
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