667865-69-2
Chemical Structure
TS-021
- CAS No.: 667865-69-2
- Formula:C17H24FN3O5S
- Molecular Weight:401.45
IUPAC Name: (2S,4S)-4-fluoro-1-((1-hydroxy-2-methylpropan-2-yl)glycyl)pyrrolidine-2-carbonitrile benzenesulfonate
InChIKey: BMWITAUNXBHIPO-OZZZDHQUSA-N
SMILES: CC(CO)(NCC(N1C[C@@H](F)C[C@H]1C#N)=O)C.O=S(C2=CC=CC=C2)(O)=O
Biological Activity: 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].
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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. | |||||||||||||||||||||
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References
- [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]
