TS-021

TS-021 is a selective, orally active, reversible and long-acting DPP-IV inhibitor, and exhibits significant inhibition selectivity against DPP-8 (> 600 fold), DPP-9 (> 1200 fold) and other peptidases (> 15,000 fold) . TS-021 inhibits DPP-IV activity in human plasma with an IC50 value of 5.34 nM. TS-021 has long-term persistent plasma drug concentration and potent antihyperglycemic activity, and increases in the active form of GLP-1[1][2].

Product Specifications

CAS Number

[667865-69-2]

UNSPSC

12352005

Target

Dipeptidyl Peptidase

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease

Applications

Metabolism-protein/nucleotide metabolism

Field of Research

Metabolic Disease

Assay Protocol

https://www.medchemexpress.com/ts-021.html

Smiles

CC(CO)(NCC(N1C[C@@H](F)C[C@H]1C#N)=O)C.O=S(C2=CC=CC=C2)(O)=O

Molecular Formula

C17H24FN3O5S

Molecular Weight

401.45

References & Citations

[1]Fukushima H, et al. Synthesis and structure-activity relationships of potent 4-fluoro-2-cyanopyrrolidine dipeptidyl peptidase IV inhibitors. Bioorg Med Chem. 2008 Apr 1;16 (7) :4093-106.|[2]Tajima A, et al. (2S,4S) -4-Fluoro-1-{[ (2-hydroxy-1,1-dimethylethyl) amino]acetyl}-pyrrolidine-2-carbonitrile monobenzenesulfonate (TS-021) is a selective and reversible dipeptidyl peptidase IV inhibitor. Eur J Pharmacol. 2011 Mar 25;655 (1-3) :99-107.