FSLLRY-NH2 TFA

Catalog No.S9915 Batch:S991501

Technical Data

Formula	C₄₁H₆₁F₃N₁₀O₁₀
Molecular Weight	910.98	CAS No.	245329-02-6 (free base)
Solubility (25°C)*	In vitro	DMSO	100 mg/mL (109.77 mM)
		Water	50 mg/mL (54.88 mM)
		Ethanol	7 mg/mL (7.68 mM)
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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

In vivo

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

Protocol (from reference)

Cell Assay:^{<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 Study:^{<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.

Cell Assay:^{<a class="sref" href="#s_ref">[1]</a>}

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 Study:^{<a class="sref" href="#s_ref">[2]</a>}

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

References

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SHIPPING AND STORAGE
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