Trelagliptin (CAS 865759-25-7) is a potent, selective dipeptidyl peptidase-4 (DPP-4) inhibitor developed for the treatment of type 2 diabetes mellitus. Chemically known as 2-[[6-[(3R)-3-aminopiperidin-1-yl]-3-methyl-2,4-dioxo-1,2,3,4-tetrahydropyrimidin-1-yl]methyl]-4-fluorobenzonitrile, Trelagliptin features a uracil core substituted with an aminopiperidine and a fluorobenzonitrile moiety.
Trelagliptin is a selective DPP-4 inhibitor and certified reference standard developed for the treatment of type 2 diabetes mellitus. As the active pharmaceutical ingredient marketed as Zafatek® in Japan, Trelagliptin provides effective glycemic control through a once-weekly dosing regimen. In pharmaceutical quality control contexts, Trelagliptin serves as the primary reference standard for impurity profiling, analytical method development, and regulatory submissions. Trelagliptin is recognized through multiple regulatory designations including INN, USAN, and JAN, making it indispensable for ANDA filings and quality control testing. The drug substance Trelagliptin exhibits excellent stability when stored under recommended conditions. Furthermore, Trelagliptin is a potent inhibitor of DPP-4 with an IC₅₀ of 3.9 nM, demonstrating the exceptional potency of this well-characterized molecular scaffold.
Product Parameters
Parameter
Specification
Product Name
Trelagliptin
CAS Number
865759-25-7
Molecular Formula
C₁₈H₂₀FN₅O₂
Molecular Weight
357.38 g/mol
Appearance
White solid
Boiling Point
519.0 ± 60.0 °C
Density
1.38 ± 0.1 g/cm3
Storage Condition
–20°C, protect from light
Synthetic Route
Trelagliptin, with the chemical name 2-[{6-[(3R)-3-amino-piperidine-1-yl]-3-methyl-2,4-dioxo-3,4-dihydro-pyrimidin-1(2H)-yl}-methyl]-4-fluorobenzonitrile, is an effective dipeptidyl peptidase IV (DPP-4) inhibitor developed by Takeda Pharmaceutical Company Limited in Japan. By selectively and persistently inhibiting DPP-4, trelagliptin helps control blood glucose levels. Trelagliptin demonstrates excellent safety and tolerability; a once-weekly dosing regimen can effectively manage blood glucose levels and improve patient adherence to treatment. It is indicated for the treatment of type 2 diabetes mellitus.
Bioactivity
Trelagliptin (SYR-472) is a highly selective long-acting DPP-4 inhibitor.
Product Advantages
Once-Weekly DPP-4 Inhibitor
Trelagliptin is a highly potent DPP-4 inhibitor with an IC₅₀ of 3.9 nM, enabling once-weekly oral administration. This extended dosing interval offers significant advantages over once-daily DPP-4 inhibitors in improving patient adherence to anti-diabetic therapy.
Highly Potent and Selective
The molecular structure of Trelagliptin confers exceptional potency and selectivity for DPP-4, ensuring effective glycemic control with minimal off-target effects.
Clinically Validated Efficacy
Trelagliptin is approved in Japan as Zafatek® for the treatment of type 2 diabetes, validating its safety and efficacy in clinical practice.
Dual-Use: API and Reference Standard
Cosperpharm supplies Trelagliptin at high-purity grade for use in both research applications and as an analytical reference standard for method development and quality control programs.
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