Wuhan HHD Supply Trelagliptin Succinate CAS 1029877-94-8 Triglitastat Succinate
Product Name: Trelagliptin succinate
Synonyms: Trelagliptin Succinate (SYR-472);SYR 111472 succinate;SYR-472 succinate;Trelagliptin succinat;SYR-472 Trelagliptin succinat;Trelagliptin succinate(SRY-472);Trelagliptin succinate SYR 111472 succinate;Triglitastat succinate
CAS: 1029877-94-8
MF: C22H26FN5O6
MW: 475.48
EINECS: 627-030-2
Melting point: 168-170°C
Boiling point: 843.3±75.0 °C
Density: 1.37±0.1 g/cm3
Storage temp.: -20°C Freezer
Appearance: White Powder
Description:
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 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.
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