Trelagliptinsuccinate , 98% , 1029877-94-8

CAS NO.：1029877-94-8

Empirical Formula: C22H26FN5O6

Molecular Weight: 475.48

MDL number: MFCD22665720

PRODUCT Properties

• storage temp.: -20°C
• solubility: Soluble in DMSO
• form: Powder
• color: Off-white solid

Description and Uses

Similar to omarigliptin, trelagliptin succinate (XIX) is a highly selective, orally delivered inhibitor of DPP-4 developed by Takeda Pharmaceuticals and approved in Japan in March 2015 for the treatment of type 2 DM. Interestingly, trelagliptin is structurally similar to alogliptin, a DPP-4 inhibitor also marketed by Takeda and described in our 2010 review, differing only in the presence of a fluorine in the 5-position of the cyanobenzyl moiety. Both trelagliptin and alogliptin are potent inhibitors of DPP-4, with IC50s of 1.3 and 5.3 nM, respectively. Notably, while similar drugs are dosed once daily, trelagliptin is the first DPP-4 inhibitor approved for onceweekly dosing. Kinetic analysis has revealed that trelagliptin is a substrate-competitive, reversible, slow-binding inhibitor (t1/2 for dissociation = ca. 30 min) of DPP-4, although the dissociation time is insufficient to explain its long-acting effects. In a phase III trial, once-weekly trelagliptin (100 mg) showed similar efficacy and safety to once-daily alogliptin (25 mg) in patients with type 2 DM inadequately controlled by diet and exercise. The medicinal chemistry discovery of trelagliptin and alogliptin as well as reviews of this class of compounds have been published.

Trelagliptin succinate (SYR-472) is a selective, long acting dipeptidyl peptidase-4 (DPP-4) inhibitor. An antidiabetic agent.
Orally active DPP-4 inhibitor that produces clinically and statistically significant improvements in glycaemic control in patients with type 2 diabetes. SYR472 has a long duration of action and is well tolerated in clinical studies.

Safety

• Symbol(GHS): GHS07
• Signal word: Warning
• Hazard statements: H302-H315-H319-H335
• Precautionary statements: P261-P305+P351+P338