research use only

FSLLRY-NH2 TFA PAR inhibitor

Cat.No.S9915

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

Chemical Structure

Molecular Weight: 910.98

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: S991501 DMSO]100 mg/mL]false]Water]50 mg/mL]false]Ethanol]7 mg/mL]false Purity: 99.31%

99.31

Related Targets	Adrenergic Receptor AChR 5-HT Receptor Histamine Receptor Dopamine Receptor Ras GPR GluR Prostaglandin Receptor CXCR Adenosine Receptor P2 Receptor CCR Angiotensin Receptor Hedgehog/Smoothened S1P Receptor PKA Cannabinoid Receptor cAMP Glucagon Receptor SGLT Opioid Receptor Sigma Receptor Endothelin Receptor LTR Neurokinin Receptor Guanylate Cyclase PKG LPA Receptor OX Receptor
Related Products	Anti-PAR2 Trypsin TRAP-6 PAR2 Antibody [N9E12] AZ3451 TFLLR-NH2 Atopaxar IUN76750 I-191 SCH79797 dihydrochloride ML161 (Parmodulin 2)

Chemical Information, Storage & Stability

Molecular Weight	910.98	Formula	C₄₁H₆₁F₃N₁₀O₁₀	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	245329-02-6 (free base)	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	FSY-NH2			Smiles	CC(C)CC(NC(=O)C(CC(C)C)NC(=O)C(CO)NC(=O)C(N)CC1=CC=CC=C1)C(=O)NC(CCCNC(N)=N)C(=O)NC(CC2=CC=C(O)C=C2)C(N)=O.OC(=O)C(F)(F)F

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (109.77 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 50 mg/mL

Ethanol : 7 mg/mL

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (5.49mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.710mg/ml (0.78mM)	Taking the 1 mL working solution as an example, add 50 μL of 14.2 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	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>
References	[1] https://pubmed.ncbi.nlm.nih.gov/11805236/ [2] https://pubmed.ncbi.nlm.nih.gov/32020571/

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