| 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 |
PAR-1[1]
This peptide specifically targets and activates the Protease-Activated Receptor 1 (PAR1), also known as the thrombin receptor. PAR1 is a GPCR primarily expressed on platelets, endothelial cells, and smooth muscle cells. By binding to this receptor, the agonist peptide initiates the same signaling cascades normally triggered by thrombin, including platelet aggregation and calcium mobilization. |
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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, PAR-1 Agonist is highly active. It stimulates platelet aggregation with an EC50 of 0.8 microM in human platelets. It promotes intracellular Ca2+ mobilization and induces rapid phosphorylation of phosphodiesterase 3A (PDE3A). It also induces activation of protein kinase C isoenzymes alpha and epsilon in human HT-29 colon carcinoma cells expressing endogenous PAR1. |
| ln Vivo |
Specific in vivo activity data for this peptide is not detailed in standard databases. Based on its mechanism, administration in vivo would be expected to induce platelet aggregation and potentially lead to thrombus formation. It is rarely used systemically due to the risk of disseminated thrombosis and is typically used ex vivo or in localized experimental settings.
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| Enzyme Assay |
The specific protocol for PAR1 binding is functional rather than direct binding, as the receptor has a large ligand-binding domain. Usually, the protocol involves the use of radiolabeled high-affinity small molecule antagonists (e.g., [3H]-haTRAP). Membranes from cells expressing PAR1 are incubated with the radiolabeled antagonist and increasing concentrations of the unlabeled PAR-1 Agonist peptide. Inhibition of radioligand binding indicates that the agonist binds to the same orthosteric site.
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| Cell Assay |
The most common in vitro assay is platelet aggregation. Human platelet-rich plasma (PRP) is prepared by centrifuging whole blood at 200g for 15 minutes. PRP (250 uL) is placed in an aggregometer cuvette with a stir bar. The PAR-1 Agonist (SFLLRN) is added at a final concentration of 10-100 uM. The increase in light transmission is recorded for 5-10 minutes. The extent of aggregation is quantified as the percentage of light transmission compared to platelet-poor plasma (PPP).
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| Animal Protocol |
There is no standard in vivo protocol for this peptide due to its potent pro-thrombotic effects. For research on receptor internalization, a protocol might involve intravenous injection into anesthetized mice at very low doses (0.1-1 mg/kg) to monitor for transient platelet activation and hypotension. However, the risk of acute thromboembolism is high. Therefore, most in vivo data comes from ex vivo studies where blood is drawn after animal treatment.
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| ADME/Pharmacokinetics |
tcY-NH2 TFA is a peptide antagonist; therefore, it is expected to have very poor oral bioavailability and a very short plasma half-life (minutes) due to extensive proteolytic degradation by peptidases in the blood and liver. It is typically administered intravenously or used in ex vivo assays. The TFA salt is used to improve solubility and stability in storage.
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| Toxicity/Toxicokinetics |
Specific toxicology data is not available for this peptide. As an activator of the platelet thrombin receptor, its primary toxicity is excessive platelet aggregation leading to thrombosis (clotting). This includes risks of pulmonary embolism, myocardial infarction, or stroke. Consequently, it is handled as a hazardous biological agent requiring safety precautions to avoid accidental systemic exposure.
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| References |
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| Additional Infomation |
This peptide is a critical research tool for studying PAR1-mediated physiology and disease. It is widely used to investigate platelet activation, vascular biology, and cancer cell metastasis. The peptide sequence for human PAR1 is SFLLRN (the first 6 amino acids). There is also a mouse-specific sequence. It is often used in contrast to PAR4-specific agonists to dissect the distinct roles of PAR1 vs PAR4 in human platelets (where both are present) compared to rodent models.
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| Molecular Formula |
C35H58N10O9
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|---|---|
| Molecular Weight |
762.896627902985
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| Exact Mass |
762.438
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| CAS # |
141136-85-8
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| Related CAS # |
Protease-Activated Receptor-1, PAR-1 Agonist TFA
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| PubChem CID |
91213358
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| Appearance |
White to off-white solid powder
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| LogP |
-3.4
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| Hydrogen Bond Donor Count |
11
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
24
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| Heavy Atom Count |
54
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| Complexity |
1300
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| Defined Atom Stereocenter Count |
7
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| SMILES |
[C@@H](NC(=O)[C@@H](N)[C@H](O)C)(C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@H](C(=O)O)CC(=O)N)CC1C=CC=CC=1
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| InChi Key |
HIKQWJFKUWYBNJ-GSAYKZDLSA-N
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| InChi Code |
InChI=1S/C35H58N10O9/c1-18(2)14-23(30(49)41-22(12-9-13-40-35(38)39)29(48)45-26(34(53)54)17-27(36)47)42-31(50)24(15-19(3)4)43-32(51)25(16-21-10-7-6-8-11-21)44-33(52)28(37)20(5)46/h6-8,10-11,18-20,22-26,28,46H,9,12-17,37H2,1-5H3,(H2,36,47)(H,41,49)(H,42,50)(H,43,51)(H,44,52)(H,45,48)(H,53,54)(H4,38,39,40)/t20-,22+,23+,24+,25+,26+,28+/m1/s1
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| Chemical Name |
(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-amino-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-4-oxobutanoic acid
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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 (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 1.3108 mL | 6.5539 mL | 13.1079 mL | |
| 5 mM | 0.2622 mL | 1.3108 mL | 2.6216 mL | |
| 10 mM | 0.1311 mL | 0.6554 mL | 1.3108 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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