TS-021

• Description:

  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].

• 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.

• Shipping Conditions:

  Room temperature

• Scientific Category:

  Reference compound1

• Clinical Information:

  No Development Reported

• Isoform:

  DPP-4

• CAS Number:

  667865-69-2