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Products
Pharmacology
Type
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- Technical support
- Resources
TFLLR-NH2
Cat. No. PR-040
Structure:
Thr-Phe-Leu-Leu-Arg-NH2
Other Names:
PAR1-AP
Activity:
PAR1 selective agonist
TFLLR-NH2 is a peptide derived from the protease activated receptor 1 (PAR1) that acts as a PAR1 selective agonist, with an EC50 of 1.9 μM. TFLLR-NH2 is widely used to activate platelets and has also been shown to elicit scratching in mice. Platelet activation of SW620 colon cancer cells with TFLLR-NH2 triggers TGF-β secretion, which induces epithelial-mesenchymal transition (EMT) through the downregulation of miR-200b expression. Activated platelets have a chemotactic effect on colon cancer cells mediated by the upregulation of CXCR4 on the cell surface.
Hollenberg et al (1997) Proteinase-activated receptors: structural requirements for activity, receptor cross-reactivity, and receptor selectivity of receptor-activating peptides. Can.J.Physiol.Pharmacol. 75 832 PMID: 9315351
Mihara et al (2013) Neutrophil elastase and proteinase-3 trigger G protein-biased signaling through proteinase-activated receptor-1 (PAR1). J Biol Chem. 288(46) 32979 PMID: 24052258
Jia et al (2015) Activation of platelet protease-activated receptor-1 induces epithelial-mesenchymal transition and chemotaxis of colon cancer cell line SW620. Oncology Reports 33(6) 2681 PMID: 25846512
Related data
All peptides >
All protease activated receptors >
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Technical Data
| Structure | Thr-Phe-Leu-Leu-Arg-NH2 |
| CAS Number | 197794-83-5 |
| Molecular Weight | 647.82 |
| Formula | C31H53N9O6 |
| Sequence | TFLLR-NH2 |
| Modifications | C-terminal amide |
Solubility and Storage
| Solubility | Soluble to 1 mg/ml in water |
| Appearance | Freeze dried solid |
| Storage | Store dry, frozen and in the dark |
Batch Specific Data
| Purity | >95% by hplc |
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Recent citations
A new publication from the University of Ljubljana uses MCA-AVLQSGFR-Lys(Dnp)-Lys-NH2, the FRET substrate for the severe acute respiratory syndrome coronavirus main protease (SARS-CoV Mpro), to determine the inhibitory potential of plant polyphenols
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