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.
For research use only. We do not sell to patients.
- CAS No.: 667865-69-2
- Formula: C17H24FN3O5S
- Molecular Weight:401.45
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[2]|
DPP-4 |
Chemical Information
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CAS No. 667865-69-2
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Molecular Weight 401.45
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Formula C17H24FN3O5S
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SMILES
CC(CO)(NCC(N1C[C@@H](F)C[C@H]1C#N)=O)C.O=S(C2=CC=CC=C2)(O)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)