| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| Other Sizes |
| Targets |
PAR2
FSLLRY-NH2 TFA targets protease-activated receptor 2 (PAR2) as a competitive antagonist. It also exhibits off-target agonistic activity on Mas-related G protein-coupled Receptor C11 (MrgprC11) with an EC50 of 10.1 μM. Its primary mechanism involves binding to the ligand-binding pocket of PAR2, thereby preventing the tethered ligand from activating the receptor. |
|---|---|
| ln Vitro |
In vitro, FSLLRY-NH2 TFA blocks trypsin-mediated PAR2 activation with an IC50 of approximately 50 μM in PAR2-expressing KNRK cell calcium-signaling assays. It suppresses ERK activation and collagen production in isolated cardiac fibroblasts. The compound does not itself activate the receptor.
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| ln Vivo |
Following asphyxial CA (asphyxial brain injury), treatment with FSLLRY-NH2 (50 μg per rat given intranasally at 1 hour postresuscitation) dramatically improves neurological outcome and decreases the amount of degenerating hippocampus neurons[1].
In vivo, FSLLRY-NH2 TFA reverses taxol-induced mechanical allodynia, heat hyperalgesia, and PKC activation in ICR mice. This demonstrates its potential as a therapeutic agent for pain management and its utility in studying PAR2-mediated pain pathways. |
| Enzyme Assay |
Non-cellular binding assays for FSLLRY-NH2 TFA involve measuring its binding affinity to PAR2. These assays can be performed using radioligand binding techniques or surface plasmon resonance (SPR) with purified PAR2 protein or membrane preparations expressing the receptor.
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| Cell Assay |
In vitro cellular assays for FSLLRY-NH2 TFA are performed using PAR2-expressing cells such as KNRK cells. Cells are treated with the compound, and its ability to inhibit trypsin-induced calcium signaling is measured. IC50 values are determined from dose-response curves.
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| Animal Protocol |
In vivo animal experiments for FSLLRY-NH2 TFA are conducted in mouse models of pain, such as taxol-induced mechanical allodynia and heat hyperalgesia models. The compound is administered via appropriate routes, and endpoints include assessment of pain behavior and PKC activation.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties for FSLLRY-NH2 TFA are not detailed in available sources. The compound has a molecular weight of 910.98 and a molecular formula of C41H61F3N10O10. Its CAS number for the free base is 245329-02-6. It is soluble in DMSO (≥115 mg/mL) and water (≥5.19 mg/mL with ultrasonic).
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| Toxicity/Toxicokinetics |
Toxicological data for FSLLRY-NH2 TFA are not provided in available sources. As a research peptide, its safety profile has not been extensively characterized. It is intended for research use only and not for human consumption.
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| References | |
| Additional Infomation |
FSLLRY-NH2 TFA is a selective PAR2 peptide antagonist that reverses taxol-induced mechanical allodynia and heat hyperalgesia in ICR mice. It also suppresses ERK activation and collagen production in isolated cardiac fibroblasts. It is supplied for research purposes only.
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| Molecular Formula |
C41H61F3N10O10
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|---|---|
| Molecular Weight |
910.98
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| Related CAS # |
FSLLRY-NH2;245329-02-6
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| Appearance |
White to off-white solid powder
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO :~100 mg/mL (~109.77 mM)
H2O :~1.43 mg/mL (~1.57 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (2.74 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (2.74 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (2.74 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 8.33 mg/mL (9.14 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.0977 mL | 5.4886 mL | 10.9772 mL | |
| 5 mM | 0.2195 mL | 1.0977 mL | 2.1954 mL | |
| 10 mM | 0.1098 mL | 0.5489 mL | 1.0977 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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