| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 100mg | |||
| Other Sizes |
| Targets |
PAR-1 thrombin receptor
Protease-activated receptor 1 (PAR-1), a G-protein-coupled receptor activated by thrombin. TRAP-6 amide acts as a peptide agonist, directly binding to and activating PAR-1, thereby triggering downstream signaling pathways including Galphaq-mediated phospholipase C activation, calcium mobilization, and protein kinase C (PKC) activation. |
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| ln Vitro |
Researchers have studied the effects of different platelet agonists on phosphatidylserine (PS) exposure and clotting times in blood without anticoagulants. Similar reductions in clotting time were obtained for collagen, TRAP-6 or calcium ionophore A23187 (50 micro mol/L), in spite of huge differences in PS expression [6.7 +/- 2.4%, 2.3 +/- 0.5% and 99.9 +/- 0.1%, respectively (mean +/- SD, n = 5)]. Furthermore, the clotting times were much longer for samples with A23187 exposing the same amounts of PS as samples with collagen or TRAP-6. Annexin V reversed the clotting time reduction, but could not prevent coagulation. Addition of phospholipid vesicles containing 20% PS neither affected the clotting times nor induced clotting in recalcified, platelet-free plasma. We conclude that platelet PS exposure is necessary, but not sufficient, for the coagulation amplification observed when platelets are stimulated via physiological receptors in a whole blood environment[1].
TRAP-6 amide potently activates PAR-1 in various cell types. It induces platelet aggregation in vitro with an EC50 of 0.15 uM. At 30 uM, it induces relaxation of isolated guinea pig internal anal sphincter strips. At 50 uM, it increases cigarette smoke extract-induced IL-8 release from isolated human bronchial epithelial cells. The peptide promotes intracellular Ca2+ mobilization and induces rapid phosphodiesterase 3A (PDE3A) phosphorylation. It activates PAR-1 independently of proteolysis, triggering downstream signaling pathways such as Galphaq-mediated phospholipase C activation. |
| ln Vivo |
In vivo, TRAP-6 amide has been used to study pain processing: intrathecal injection in mice produces anti-hyperalgesic effects, mimicking the effects of thrombin in inhibiting NMDA-induced pain behaviors. It also induces platelet aggregation and thrombosis in animal models when administered systemically, making it useful for studying thrombotic disorders and evaluating antiplatelet agents. The peptide induces transient effects due to its short half-life in circulation.
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| Enzyme Assay |
PAR-1 receptor binding assay: Membranes from cells expressing PAR-1 (e.g., CHRF-288-11 megakaryocytic cells or HEK293-PAR1 transfectants) are incubated with a radiolabeled PAR-1 antagonist or a fluorescently labeled TRAP peptide analog and varying concentrations of TRAP-6 amide (0.01-10,000 nM) in binding buffer (50 mM HEPES pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) for 1-2 hours at room temperature. Bound radioactivity/fluorescence is measured to determine binding affinity and competition.
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| Cell Assay |
Calcium mobilization assay: Cells expressing PAR-1 (e.g., platelets, CHRF-288-11 cells, or HEK293-PAR1 transfectants) are loaded with a calcium-sensitive fluorescent dye (Fluo-4 AM, 2-5 uM) for 30-60 minutes at 37degC. After washing, cells are plated in 96-well plates and TRAP-6 amide (0.001-100 uM) is added. Calcium flux (increase in fluorescence, excitation 485 nm, emission 525 nm) is measured using a FLIPR or fluorescence plate reader. The EC50 for receptor activation is calculated from dose-response curves. Platelet aggregation assay: Platelet-rich plasma (PRP) is prepared from human or animal blood by centrifugation. PRP is pre-warmed to 37degC in an aggregometer cuvette with stirring, and TRAP-6 amide (0.01-100 uM) is added. Aggregation is monitored by increase in light transmission. EC50 for aggregation is determined.
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| Animal Protocol |
Mouse models of pain: TRAP-6 amide is administered intrathecally (e.g., 1-10 nmol in 5 uL saline) to mice, and its effect on nociceptive behaviors is assessed using the formalin test or von Frey test for mechanical allodynia. The peptide's anti-hyperalgesic effects are measured by reduction in pain-related behaviors. Models of thrombosis: The peptide is administered intravenously to induce platelet aggregation and evaluate antithrombotic agents; platelet count and thrombus formation are monitored.
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| ADME/Pharmacokinetics |
As a peptide, TRAP-6 amide is rapidly degraded in vivo, with a short half-life (minutes) in circulation. It is not orally bioavailable and requires parenteral administration (intravenous, intrathecal, or intraperitoneal). The C-terminal amide provides some resistance to carboxypeptidase degradation but does not prevent endopeptidase cleavage.
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| Toxicity/Toxicokinetics |
No specific toxicity data are reported for TRAP-6 amide. As a research peptide not intended for therapeutic use, comprehensive toxicological profiling has not been performed. High doses may induce excessive platelet aggregation and thrombosis due to PAR-1 overactivation.
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| References | |
| Additional Infomation |
This is a research peptide, not an approved drug. It is a standard tool for studying PAR-1 function in hemostasis, thrombosis, inflammation, and pain. Also known as Thrombin Receptor Agonist Peptide-6 amide, PAR-1 agonist peptide, or SFLLRN-NH2. The amidated version is more potent than the free acid form (TRAP-6, EC50 = 0.8 uM).
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| Molecular Formula |
C34H57N11O8
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|---|---|
| Molecular Weight |
747.88528
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| Exact Mass |
747.439
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| CAS # |
141923-40-2
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| Related CAS # |
TRAP-6 amide TFA;1426807-16-0
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| PubChem CID |
10010285
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| Sequence |
H-Ser-Phe-Leu-Leu-Arg-Asn-NH2; L-seryl-L-phenylalanyl-L-leucyl-L-leucyl-L-arginyl-L-asparaginamide
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| SequenceShortening |
SFLLRN;
H-SFLLRN-[NH2]
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| Appearance |
White to off-white solid powder
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| LogP |
1.935
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| Hydrogen Bond Donor Count |
11
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
24
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| Heavy Atom Count |
53
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| Complexity |
1270
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| Defined Atom Stereocenter Count |
6
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| SMILES |
CC(C)C[C@@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(=O)N)C(=O)N)NC(=O)[C@H](CC1=CC=CC=C1)NC(=O)[C@H](CO)N
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| InChi Key |
HRYITGOEDRTTLM-FRSCJGFNSA-N
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| InChi Code |
InChI=1S/C34H57N11O8/c1-18(2)13-24(31(51)41-22(11-8-12-40-34(38)39)30(50)42-23(28(37)48)16-27(36)47)44-32(52)25(14-19(3)4)45-33(53)26(43-29(49)21(35)17-46)15-20-9-6-5-7-10-20/h5-7,9-10,18-19,21-26,46H,8,11-17,35H2,1-4H3,(H2,36,47)(H2,37,48)(H,41,51)(H,42,50)(H,43,49)(H,44,52)(H,45,53)(H4,38,39,40)/t21-,22-,23-,24-,25-,26-/m0/s1
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| Chemical Name |
(2S)-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-(diaminomethylideneamino)pentanoyl]amino]butanediamide
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| Synonyms |
141923-40-2; (2S)-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-(diaminomethylideneamino)pentanoyl]amino]butanediamide; L-Aspartamide, L-seryl-L-phenylalanyl-L-leucyl-L-leucyl-L-arginyl-; CHEMBL33473; (S)-2-((2S,5S,8S,11S,14S)-14-amino-11-benzyl-2-(3-guanidinopropyl)-15-hydroxy-5,8-diisobutyl-4,7,10,13-tetraoxo-3,6,9,12-tetraazapentadecanamido)succinamide; TRAP-6 amide (trifluoroacetate salt); Ser-Phe-Leu-Leu-Arg-Asn-NH2; BDBM85085;
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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 (~133.53 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 33.33 mg/mL (44.51 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 | 1.3371 mL | 6.6855 mL | 13.3710 mL | |
| 5 mM | 0.2674 mL | 1.3371 mL | 2.6742 mL | |
| 10 mM | 0.1337 mL | 0.6685 mL | 1.3371 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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