| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Protease-Activated Receptor-1, PAR-1 Agonist TFA targets the PAR-1 receptor (also known as thrombin receptor), a GPCR that is activated by proteolytic cleavage of its N-terminus by thrombin. The synthetic peptide corresponds to the tethered ligand (SFLLRN) of PAR-1 and serves as an agonist. By binding to and activating PAR-1, this peptide mimics the effects of thrombin, including platelet aggregation, endothelial cell activation, and smooth muscle cell proliferation.
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| ln Vitro |
In human HT-29 colon cancer cells that express PAR1 endogenously, protease-activated receptor-1, PAR-1 antagonist, activates protein kinase C isoenzymes alpha and epsilon. At the cellular level, HT-29 cell migration and matrix adhesion were induced by Protease-Activated Receptor-1, PAR-1 Agonist, and thrombin through a PKCepsilon-dependent mechanism. This was determined by the fact that the PKC inhibitors bisindolylmaleimide I and the PKCepsilon translocation inhibitory peptide EAVSLKPT, but not Gö 6976, inhibited the effects of PAR1-mediated processes.
In vitro, Protease-Activated Receptor-1, PAR-1 Agonist TFA induces activation of protein kinase C isoenzymes alpha and epsilon in human HT-29 colon carcinoma cells expressing PAR-1 endogenously. On the cellular level, it mimics the actions of thrombin via PAR-1. The peptide is used to study PAR-1-mediated signaling pathways, including calcium mobilization, MAPK activation, and cytoskeletal rearrangements. |
| ln Vivo |
In vivo, PAR-1 agonist peptide can be used to study the role of PAR-1 in thrombosis, inflammation, and vascular biology. By selectively activating PAR-1 without the off-target effects of thrombin, the peptide enables the dissection of PAR-1-specific pathways in animal models. It can induce platelet aggregation and endothelial activation in vivo, mimicking the pro-thrombotic effects of thrombin. This compound is a selective PAR-1 agonist.
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| Enzyme Assay |
A cell-free binding assay for PAR-1 agonist can be performed. Membranes from CHO or HEK293 cells expressing human PAR-1 are incubated with a radiolabeled antagonist (e.g., [3H]haTRAP or [3H]SCH530348) and increasing concentrations of the PAR-1 agonist peptide. Bound radioligand is separated by filtration through GF/B filters. The IC50 and Ki values are calculated. Alternatively, a functional cell-free GTPgammaS binding assay measures receptor activation.
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| Cell Assay |
HT-29 human colon carcinoma cells (which endogenously express PAR-1) are seeded in 6-well plates. After overnight culture, cells are treated with PAR-1 agonist peptide (1-100 uM) for 5-30 min. Cell lysates are prepared, and protein kinase C (PKC) activity is measured by Western blot using an anti-phospho-PKC substrate antibody. PKC isoform activation (alpha and epsilon) can be assessed using isoform-specific phospho-antibodies. Calcium mobilization can be measured using Fluo-4 AM dye.
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| Animal Protocol |
PAR-1 agonist peptide can be studied in mouse models of thrombosis. Male C57BL/6 mice (20-25 g, n=8-10 per group) are administered the PAR-1 agonist peptide intravenously (0.1-10 mg/kg in PBS). Platelet aggregation is measured by whole-blood aggregometry. Tail bleeding time is determined. In a pulmonary thrombosis model, mice are injected with the peptide, and lung histology is performed to assess platelet-rich thrombi. PAR-1 activation is expected to induce rapid thrombus formation.
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| ADME/Pharmacokinetics |
Protease-Activated Receptor-1, PAR-1 Agonist TFA has a molecular formula of C38H53F3N10O10 and a molecular weight of 866.89. The peptide corresponds to the PAR1 tethered ligand SFLLRN. It should be stored as a powder at -20degC, sealed and away from moisture. In solvent, it is stable for 6 months at -80degC. The TFA salt ensures solubility in aqueous buffers. Specific PK parameters have not been reported.
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| Toxicity/Toxicokinetics |
No detailed toxicity data are available for the PAR-1 agonist peptide. As an activator of the thrombin receptor, high doses may induce uncontrolled platelet aggregation, thrombosis, and consumptive coagulopathy. Therefore, the compound should be handled with caution and used at appropriate doses in vivo. Standard safety precautions for peptide handling should be followed.
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| References |
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| Additional Infomation |
Protease-Activated Receptor-1, PAR-1 Agonist TFA is a research-grade peptide and is not approved for clinical use. It is a selective PAR-1 agonist that corresponds to the PAR1 tethered ligand and can selectively mimic the actions of thrombin via the PAR-1 receptor. This product is a valuable research tool for studying PAR-1 signaling in thrombosis, inflammation, and vascular biology. It is for research use only.
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| Molecular Formula |
C37H59F3N10O11
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| Molecular Weight |
876.92
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| Related CAS # |
Protease-Activated Receptor-1, PAR-1 Agonist;141136-85-8
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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) |
H2O :~6.67 mg/mL (~7.61 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 5 mg/mL (5.70 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.1404 mL | 5.7018 mL | 11.4035 mL | |
| 5 mM | 0.2281 mL | 1.1404 mL | 2.2807 mL | |
| 10 mM | 0.1140 mL | 0.5702 mL | 1.1404 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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