Biological Activity
Selective PAR2 peptide antagonist. Reverses taxol-induced mechanical allodynia, heat hyperalgesia and PKC activation in ICR mice. Blocks ERK activation and collagen production in isolated cardiac fibroblasts. Also reduces symptoms in a mouse model of dermatophyte-associated itch.
Technical Data
| M. Wt | 796.97 |
| Formula | C39H60N10O8 |
| Sequence |
FSLLRY-NH2 (Modifications: Tyr-6 = C-terminal amide) |
| Storage | Store at -20°C |
| CAS Number | 245329-02-6 |
| PubChem ID | 73352412 |
| InChI Key | KMSCNWHRNILNRJ-JNRWAQIZSA-N |
| Smiles | [H]N[C@@H](CC1=CC=CC=C1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC1=CC=C(O)C=C1)C(N)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solubility | Soluble to 1 mg/ml in water |
Preparing Stock Solutions
The following data is based on the product molecular weight 796.97. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.25 mL | 6.27 mL | 12.55 mL |
| 5 mM | 0.25 mL | 1.25 mL | 2.51 mL |
| 10 mM | 0.13 mL | 0.63 mL | 1.25 mL |
| 50 mM | 0.03 mL | 0.13 mL | 0.25 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
McLarty et al (2011) Tryptase/protease-activated receptor 2 interactions induce selective mitogen-activated protein kinase signaling and collagen synthesis by cardiac fibroblasts. Hypertension 58 264 PMID: 21730297
Chen et al (2011) Proteinase-activated receptor 2 sensitizes transient receptor potential vanilloid 1, transient receptor potential vanilloid 4, and transient receptor potential ankyrin 1 in paclitaxel-induced neuropathic pain. Neuroscience 193 440 PMID: 21763756
Andoh et al (2012) Involvement of serine protease and proteinase-activated receptor 2 in dermatophyte-associated itch in mice. J.Pharmacol.Exp.Ther. 343 91 PMID: 22761302
Keywords: FSLLRY-NH2, supplier, PAR2, protease, activated, receptors, selective, antagonists, Protease-Activated, Receptors, Protease-Activated, Receptors, Tocris Bioscience
