FSLLRY-NH2 TFA

Catalog No.S9915 Synonyms: FSY-NH2

For research use only.

FSLLRY-NH2 TFA (FSY-NH2) is a selective protease-activated receptor 2 (PAR2) inhibitor with an ic50 of 50 µM in PAR2-KNRK cells.

FSLLRY-NH2 TFA Chemical Structure

CAS No. 245329-02-6 (free base)

Purity & Quality Control

Choose Selective PAR Inhibitors

Biological Activity

Description FSLLRY-NH2 TFA (FSY-NH2) is a selective protease-activated receptor 2 (PAR2) inhibitor with an ic50 of 50 µM in PAR2-KNRK cells.
Targets
PAR2 [1]
(in PAR2-KNRK cells)
50 µM
In vitro

FSLLRY-NH2 blocks the ability of trypsin to activate PAR(2) either in PAR(2)-expressing Kirsten virus-transformed kidney (KNRK) cell lines or in a rat aorta ring preparation. The mechanism of this activity does not involve a simple inhibition of trypsin proteolytic activity, but possibly by interacting with a tethered ligand receptor-docking site.<sup><a class="sref"href="#s_ref">[1]</a></sup>

In vivo

Treatment with FSLLRY-NH2 significantly improves neurological outcome and reduces the number of degenerating hippocampal neurons after ACA (asphyxial CA).<sup><a class="sref"href="#s_ref">[2]</a></sup>

Protocol (from reference)

Cell Research:

<sup><a class="sref" href="#s_ref">[1]</a></sup>

  • Cell lines: Kirsten virus-transformed kidney (KNRK) cells
  • Concentrations: 200 μM
  • Incubation Time: 1 h
  • Method:

    KNRK cells are incubated with 10 nM trypsin  at 37°C for 10 to 60 min in the presence or absence of 200 μM FSLLRY-NH2. The absorbance of the released resorufin, reflecting proteolytic activity, is measured using a Beckman DU 640B Spectrophotometer at 574 nm for assay of proteolytic activity of trypsin.

Animal Research:

<sup><a class="sref" href="#s_ref">[2]</a></sup>

  • Animal Models: ACA rat mode rats(ladult male Sprague-Dawley)
  • Dosages: 50 μg
  • Administration: i.n.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 910.98
Formula

C41H61F3N10O10

CAS No. 245329-02-6 (free base)
Storage 3 years -20°C powder
2 years -80°C in solvent

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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