| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Targets |
P4pal10 TFA specifically targets and antagonizes protease-activated receptor 4 (PAR4), a G protein-coupled receptor (GPCR) expressed on platelets and other cells. It acts as a pepducin, a cell-penetrating peptide that targets the intracellular loops of the receptor. By binding to the receptor's intracellular surface, it blocks the receptor's ability to activate its downstream G protein signaling pathways, thereby inhibiting platelet activation and aggregation.
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| ln Vitro |
In non-cell assays, P4pal10 TFA is used to study the molecular interactions between the peptide and the PAR4 receptor. Its binding affinity can be assessed using surface plasmon resonance (SPR) with purified PAR4 or membrane preparations. Direct evidence of its antagonism is typically confirmed by its ability to inhibit PAR4-mediated signaling in cell-based or functional assays (e.g., platelet aggregation), which is its primary activity readout.
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| ln Vivo |
In cell-based assays, P4pal10 TFA is a potent inhibitor of platelet aggregation. In a platelet aggregation assay, washed human platelets are pre-incubated with P4pal10 TFA (e.g., 10-100 uM) for 5 minutes. The platelets are then stimulated with a PAR4 agonist, such as AYPGKF-NH2 (100-500 uM). Platelet aggregation is measured by light transmission aggregometry. P4pal10 TFA inhibits PAR4-mediated platelet aggregation in a dose-dependent manner. It also inhibits tissue factor (TF)-induced thrombin generation.
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| Enzyme Assay |
For a non-cell binding assay, the affinity of P4pal10 TFA for PAR4 can be determined by SPR. Recombinant PAR4 protein, or a fragment of its intracellular loop, is immobilized on a sensor chip. Increasing concentrations of P4pal10 TFA are flowed over the chip. The association and dissociation phases are monitored, and the binding kinetics (ka, kd) and affinity constant (KD) are calculated. This assay confirms direct binding of the peptide to the intracellular domain of the receptor.
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| Cell Assay |
For platelet aggregation assays, human blood is collected into acid-citrate-dextrose (ACD) solution. Platelet-rich plasma (PRP) is obtained by centrifugation. The PRP is incubated with P4pal10 TFA (1-200 uM) for 5 minutes at 37degC. Platelet aggregation is initiated by adding the PAR4 agonist peptide AYPGKF-NH2 (100 uM). Aggregation is monitored for 5-10 minutes in a light transmission aggregometer, and the percentage of maximal aggregation is calculated. For thrombin generation assays, platelet-poor plasma (PPP) is spiked with tissue factor and phospholipids. P4pal10 TFA is added, and thrombin generation is measured using a calibrated automated thrombogram (CAT), which continuously monitors a fluorogenic substrate.
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| Animal Protocol |
The in vivo efficacy of P4pal10 TFA has been demonstrated in mouse models. In one study, the compound was shown to reduce carrageenan-induced paw edema and granulocyte infiltration, indicating anti-inflammatory activity. In a standard protocol, male BALB/c mice were administered P4pal10 TFA (e.g., 1-10 mg/kg, IP) 30 minutes before a sub-plantar injection of carrageenan (1% in saline). Paw swelling was measured for several hours. In thrombosis models, P4pal10 TFA has been shown to exhibit antithrombotic activity, but detailed protocols are not publicly available.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for P4pal10 TFA is not publicly available. As a peptide, it is not expected to be orally bioavailable. It is typically administered by parenteral routes (e.g., intraperitoneal injection, IV) for in vivo studies. Its plasma half-life is likely short, as it would be subject to proteolytic degradation. For research use, it is stored as a lyophilized powder at -20degC or -80degC, protected from light and moisture.
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| Toxicity/Toxicokinetics |
Specific toxicity data for P4pal10 TFA is not publicly available. Based on its mechanism as an antithrombotic agent, potential off-target toxicities could include an increased risk of bleeding. As a research chemical, it is intended for laboratory use only and should be handled with standard precautions. Appropriate PPE (gloves, lab coat) should be worn.
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| References |
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| Additional Infomation |
P4pal10 TFA is a research-grade peptide and is not an FDA-approved drug. It has no approved clinical use. It is a valuable pharmacological tool for studying the role of PAR4 in platelet function, thrombosis, and inflammation. PAR4 is considered a promising target for novel antiplatelet therapies, and P4pal10 is an important tool for validating this target.
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| Molecular Formula |
C65H112N22O13.XC2HF3O2
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| Molecular Weight |
1409.72 (free base)
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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: (1). 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 (with ultrasonication)
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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.) |
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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