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Trelagliptin

Names

[ CAS No. ]:
865759-25-7

[ Name ]:
Trelagliptin

[Synonym ]:
Trelagliptin (USAN)
2-({6-[(3R)-3-Amino-1-piperidinyl]-3-methyl-2,4-dioxo-3,4-dihydro-1(2H)-pyrimidinyl}methyl)-4-fluorobenzonitrile
Trelagliptin
UNII-Q836OWG55H
Benzonitrile, 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]-4-fluoro-
SYR 472

Biological Activity

[Description]:

Trelagliptin(SYR-472) is a long acting dipeptidyl peptidase-4 (DPP-4) inhibitor that is being developed for the treatment of type 2 diabetes (T2D). IC50 value:Target: DPP4Two Phase II clinical studies have been completed with Efficacy and Safety of SYR-472 in Subjects With Type 2 Diabetes Mellitus. Phase III clinical studies with trelagliptin in Japan to evaluate its safety and efficacy in a once-weekly oral treatment regimen. Currently, all available DPP-4 inhibitors are dosed once-daily. A once-weekly treatment, such as trelagliptin, would provide patients with a convenient treatment alternative and has the potential to improve treatment compliance.

[Related Catalog]:

Signaling Pathways >> Metabolic Enzyme/Protease >> Dipeptidyl Peptidase
Research Areas >> Metabolic Disease

[References]

[1]. Efficacy of SYR-472 in Subjects With Type 2 Diabetes Mellitus

[2]. Efficacy and Safety of SYR-472 in Subjects With Type 2 Diabetes Mellitus

[3]. Long-term Study of SYR-472

[4]. SYR-472 Open-label Study


[Related Small Molecules]

Talabostat mesylate | Linagliptin | Teneligliptin | Vildagliptin (LAF-237) | AZD7986 | Omarigliptin | Anagliptin | Gemigliptin | Trelagliptin succinate | DPP-IV-IN-2 | DBPR108 | Diprotin A TFA (Ile-Pro-Pro (TFA)) | Saikogenin A | UAMC 00039 dihydrochloride | Dutogliptin

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Boiling Point ]:
519.0±60.0 °C at 760 mmHg

[ Molecular Formula ]:
C18H20FN5O2

[ Molecular Weight ]:
357.382

[ Flash Point ]:
267.7±32.9 °C

[ Exact Mass ]:
357.160095

[ PSA ]:
97.05000

[ LogP ]:
1.88

[ Vapour Pressure ]:
0.0±1.4 mmHg at 25°C

[ Index of Refraction ]:
1.646

[ Storage condition ]:
-20°C

[ Water Solubility ]:
Practically insoluble (0.034 g/L) (25 ºC)


Related Compounds