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| 10mg |
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| Targets |
SFLLRNPNDKYEPF targets the protease-activated receptor 1 (PAR-1), also known as the thrombin receptor. As a synthetic peptide agonist, it binds to and activates PAR-1 without requiring proteolytic cleavage by thrombin. The peptide mimics the tethered ligand that is exposed after thrombin-mediated cleavage of the receptor's extracellular N-terminus. PAR-1 is a G protein-coupled receptor that plays a critical role in platelet activation, coagulation, inflammation, and vascular biology. The compound has IC₅₀ values in the nanomolar to micromolar range depending on the assay system and cell type used.
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| ln Vitro |
At arginine 41, thrombin cleaves its receptor, creating a new receptor NH2 terminus containing the sequence TRAP-14. Multiple thrombin reactions may be signaled by this peptide (TRAP-14) [1]. It was discovered that TRAP-14, which stands for the 14 amino acids beginning with the human thrombin receptor Ser-42, mimics the effects of thrombin on platelets. A novel N terminus that functions as a potential tethering ligand is revealed upon thrombin's cleavage of the human platelet thrombin receptor. The novel N-terminal region known as TRAP-14 is responsible for activating and inducing serotonin secretion and platelet aggregation. The smallest peptide length that can still fully induce [14C]serotonin secretion is TRAP-14 [2]. HUVEC underwent fast morphological changes as a result of TRAP, and prostacyclin, endothelin, platelet-activating factor, tissue plasminogen activator, and plasminogen activator inhibitor 1 were released in significantly higher amounts. Cell surface thrombomodulin also rapidly decreases when cells are incubated with TRAP [3].
In vitro, SFLLRNPNDKYEPF activates platelets and induces platelet aggregation and serotonin secretion. It induces rapid morphological changes in human umbilical vein endothelial cells (HUVECs), with marked increases in the release of prostacyclin, endothelin, platelet-activating factor, tissue-type plasminogen activator, and plasminogen activator inhibitor-1. The peptide also stimulates intracellular calcium mobilization, MAP kinase activation, and receptor internalization in PAR-1-expressing cells. It is a potent activator of PAR-1-mediated signaling pathways, including Gαq/11, Gα12/13, and Gαi/o pathways, leading to diverse cellular responses depending on the cell type. |
| ln Vivo |
In vivo, SFLLRNPNDKYEPF has been used to study thrombin receptor-mediated effects in animal models. Administration of the peptide in rodent models induces platelet aggregation and thrombus formation, mimicking the effects of thrombin. It has been used to investigate the role of PAR-1 in vascular inflammation, vascular permeability, and thrombosis. The peptide's effects in vivo are typically transient due to rapid proteolytic degradation by peptidases. However, specific in vivo data for SFLLRNPNDKYEPF are limited, and most studies have focused on its in vitro applications for elucidating PAR-1 signaling mechanisms.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for SFLLRNPNDKYEPF typically involve radioligand binding studies using membranes from cells expressing human PAR-1. The peptide is incubated with increasing concentrations of radiolabeled ligand (e.g., ³H-haTRAP) in binding buffer containing protease inhibitors to prevent peptide degradation. Nonspecific binding is determined in the presence of excess unlabeled peptide. Following incubation at room temperature for 60-120 minutes, bound and free ligand are separated by rapid filtration through glass fiber filters, and bound radioactivity is measured by scintillation counting. Competition binding curves are generated, and IC₅₀ values are calculated by nonlinear regression analysis.
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| Cell Assay |
In vitro cell-based assays for SFLLRNPNDKYEPF typically employ PAR-1-expressing cells such as human platelets, HUVECs, or transfected cell lines (e.g., CHO-K1 cells stably expressing human PAR-1). Cells are treated with various concentrations of the peptide (typically 0.1-100 μM) for various time periods. Platelet aggregation is measured by light transmission aggregometry, and serotonin release is quantified by radioimmunoassay or ELISA. Calcium mobilization is measured using fluorescent calcium indicators such as Fluo-4 or Fura-2. MAP kinase activation is assessed by Western blot analysis of phosphorylated ERK1/2. Receptor internalization is evaluated by immunofluorescence microscopy or flow cytometry.
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| Animal Protocol |
In vivo animal studies with SFLLRNPNDKYEPF typically involve intravenous or intraperitoneal administration to rodents at doses ranging from 0.1 to 10 mg/kg. Blood samples are collected at various time points for platelet count analysis and measurement of platelet aggregation ex vivo. Thrombus formation is assessed in models such as the ferric chloride-induced carotid artery injury model or the pulmonary embolism model. Vascular permeability is evaluated by Evans blue dye extravasation assay. Tissue samples are collected for histological examination and immunohistochemical analysis of PAR-1 expression and activation markers.
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| ADME/Pharmacokinetics |
Pharmacokinetic (PK) properties of SFLLRNPNDKYEPF are characterized by rapid clearance from the circulation due to proteolytic degradation by peptidases. Following intravenous administration, the peptide has a short half-life, typically in the range of minutes, due to rapid metabolism by serum and tissue peptidases. The compound is not orally bioavailable and requires parenteral administration for in vivo studies. It is distributed primarily in the blood and vascular compartments, with limited penetration into tissues. Metabolism occurs via cleavage of peptide bonds by various proteases, and the peptide fragments are excreted in urine. No specific PK data for SFLLRNPNDKYEPF are available in the published literature.
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| Toxicity/Toxicokinetics |
The toxicity profile of SFLLRNPNDKYEPF has not been extensively characterized in preclinical studies. As a peptide agonist of PAR-1, the compound's primary toxicities are expected to relate to its pharmacological activity, including excessive platelet activation, thrombosis, and vascular inflammation. At high doses, the peptide may induce disseminated intravascular coagulation or thrombotic complications. No specific toxicology studies have been published for this compound. The compound is intended for research use only and is not approved for human therapeutic applications. Standard safety precautions should be followed when handling this peptide.
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| References |
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| Additional Infomation |
SFLLRNPNDKYEPF (TRAP-14) is a research-grade peptide agonist of the thrombin receptor PAR-1. It is not an approved therapeutic drug and has no clinical trial history or regulatory approval for human use. The peptide is widely used as a pharmacological tool to study PAR-1 signaling, platelet activation, thrombosis, and vascular biology. It is supplied as a lyophilized powder with purity ≥97% (HPLC) and should be stored at -20°C for long-term stability. The compound is soluble in water and aqueous buffers. Sequence: SFLLRNPNDKYEPF. Synonyms include Thrombin Receptor Agonist Peptide, TRAP-14, and SFLLRNPNDKYEPF.
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| Molecular Formula |
C81H118N20O23
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|---|---|
| Molecular Weight |
1739.92000
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| Exact Mass |
1738.87
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| CAS # |
137339-65-2
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| PubChem CID |
16131180
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| Appearance |
White to off-white solid powder
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| LogP |
2.881
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| Hydrogen Bond Donor Count |
23
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| Hydrogen Bond Acceptor Count |
26
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| Rotatable Bond Count |
54
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| Heavy Atom Count |
124
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| Complexity |
3670
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| Defined Atom Stereocenter Count |
14
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| SMILES |
CC(C)C[C@@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)N)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC2=CC=C(C=C2)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N3CCC[C@H]3C(=O)N[C@@H](CC4=CC=CC=C4)C(=O)O)NC(=O)[C@H](CC5=CC=CC=C5)NC(=O)[C@H](CO)N
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| InChi Key |
OXHYRVSBKWIFES-WWSDOYNLSA-N
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| InChi Code |
InChI=1S/C81H118N20O23/c1-43(2)34-53(93-71(114)54(35-44(3)4)94-73(116)55(92-67(110)49(83)42-102)36-45-16-7-5-8-17-45)70(113)90-51(21-13-31-88-81(86)87)69(112)98-59(40-64(85)105)79(122)101-33-15-22-61(101)76(119)97-57(39-63(84)104)74(117)96-58(41-66(108)109)75(118)89-50(20-11-12-30-82)68(111)95-56(37-47-24-26-48(103)27-25-47)72(115)91-52(28-29-65(106)107)78(121)100-32-14-23-62(100)77(120)99-60(80(123)124)38-46-18-9-6-10-19-46/h5-10,16-19,24-27,43-44,49-62,102-103H,11-15,20-23,28-42,82-83H2,1-4H3,(H2,84,104)(H2,85,105)(H,89,118)(H,90,113)(H,91,115)(H,92,110)(H,93,114)(H,94,116)(H,95,111)(H,96,117)(H,97,119)(H,98,112)(H,99,120)(H,106,107)(H,108,109)(H,123,124)(H4,86,87,88)/t49-,50-,51-,52-,53-,54-,55-,56-,57-,58-,59-,60-,61-,62-/m0/s1
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| Chemical Name |
(4S)-4-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-1-[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-3-hydroxypropanoyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-oxobutanoyl]pyrrolidine-2-carbonyl]amino]-4-oxobutanoyl]amino]-3-carboxypropanoyl]amino]hexanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-5-[(2S)-2-[[(1S)-1-carboxy-2-phenylethyl]carbamoyl]pyrrolidin-1-yl]-5-oxopentanoic 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, 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 (~57.47 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (1.44 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 (1.44 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 (1.44 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: 50 mg/mL (28.74 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 | 0.5747 mL | 2.8737 mL | 5.7474 mL | |
| 5 mM | 0.1149 mL | 0.5747 mL | 1.1495 mL | |
| 10 mM | 0.0575 mL | 0.2874 mL | 0.5747 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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