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].

401.45

C₁₇H₂₄FN₃O₅S

667865-69-2

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

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]

  [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.   [Content Brief]