| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
PAR-3[1]
Protease-Activated Receptor-3 (PAR-3) (1-6), human TFA targets the PAR-3 receptor, a member of the protease-activated receptor family of GPCRs. PAR-3 functions as a cofactor for thrombin-mediated activation of PAR-4 on platelets, facilitating efficient cleavage and activation. PAR-3 enhances thrombin's ability to activate PAR-4, playing a critical role in hemostasis. The peptide is an agonist of PAR-3. |
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| ln Vitro |
In vitro, Protease-Activated Receptor-3 (PAR-3) (1-6), human TFA acts as an agonist for the protease-activated receptor-3 (PAR-3). It can be used to study PAR-3-mediated signaling pathways. PAR-3 has been identified as a critical cofactor in hemostasis, enhancing thrombin's ability to activate PAR-4 on platelets. The peptide is a valuable tool for dissecting PAR family functions in pain signaling pathways and hemostasis.
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| ln Vivo |
In vivo, PAR-3 has been identified as a critical cofactor in hemostasis. The PAR-3 (1-6) agonist peptide can be used to study the role of PAR-3 in platelet activation and clotting. Additionally, lipid-tethered agonists for PAR-3 have been developed to investigate its function in pain signaling pathways. The peptide is suitable for in vivo administration to explore PAR-3 biology.
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| Enzyme Assay |
A cell-free binding assay for PAR-3 is not typical; functional assays are more common. For receptor binding, membranes from cells expressing human PAR-3 (HEK293-PAR3) are used. Membranes (10-20 ug protein) are incubated with a radiolabeled PAR-3 agonist (if available) and increasing concentrations of PAR-3 (1-6) peptide. Bound radioligand is separated by filtration. Alternatively, a TR-FRET-based assay using labeled receptor and ligand can be developed.
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| Cell Assay |
HEK293 cells stably expressing human PAR-3 receptor are seeded in 96-well plates. Cells are loaded with Fluo-4 AM calcium dye. PAR-3 (1-6), human TFA peptide is added at varying concentrations (0.01-100 uM). The increase in intracellular calcium is measured as a proxy for receptor activation. The EC50 is calculated. Specificity can be confirmed by using a PAR-3 antagonist or by testing the peptide on cells expressing other PAR family members (PAR-1, PAR-2, PAR-4).
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| Animal Protocol |
Protease-Activated Receptor-3 (PAR-3) (1-6), human TFA can be studied in mouse models to evaluate its effects on hemostasis and platelet function. Male C57BL/6 mice are used. The peptide is administered intravenously (1-10 mg/kg in PBS). Tail bleeding time is measured as a readout of platelet function. Blood samples are collected, and platelet aggregation is assessed using an aggregometer. In models of thrombosis, the peptide may be tested for its ability to modulate clot formation.
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| ADME/Pharmacokinetics |
Protease-Activated Receptor-3 (PAR-3) (1-6), human TFA has a molecular formula of C31H47F3N10O9 and a molecular weight of 760.76. The peptide is typically a solid at room temperature. It should be stored as a powder at -80degC for up to 2 years or at -20degC for 1 year, sealed and away from moisture. In solvent, it is stable for 6 months at -80degC or 1 month at -20degC. The TFA salt enhances solubility.
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| Toxicity/Toxicokinetics |
No detailed toxicity data are available for PAR-3 (1-6) peptide. As a short peptide agonist, it is expected to have low inherent toxicity. Standard safety precautions for peptide handling should be followed. At high concentrations, PAR-3 activation may cause excessive platelet activation and thrombosis. However, formal toxicity studies have not been reported.
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| References | |
| Additional Infomation |
Protease-Activated Receptor-3 (PAR-3) (1-6), human TFA is a research-grade peptide agonist of the protease-activated receptor 3 (PAR-3). It is a valuable tool for studying PAR-3 function in hemostasis, platelet activation, and pain signaling. This product is for research use only and is not approved for clinical or therapeutic use.
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| Molecular Formula |
C31H47F3N10O9
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| Molecular Weight |
760.76
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| Related CAS # |
Protease-Activated Receptor-3 (PAR-3) (1-6), human;1872435-09-0
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| Appearance |
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) |
H2O :~100 mg/mL (~131.45 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.3145 mL | 6.5724 mL | 13.1447 mL | |
| 5 mM | 0.2629 mL | 1.3145 mL | 2.6289 mL | |
| 10 mM | 0.1314 mL | 0.6572 mL | 1.3145 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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