TRAP-6 (Synonyms: PAR-1 agonist peptide; Thrombin Receptor Activator Peptide 6) |
| Katalog-Nr.GC11662 |
TRAP-6 (PAR-1-Agonist-Peptid), ein Peptidfragment, ist ein selektiver Protease-aktivierender Rezeptor 1 (PAR1)-Agonist.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 141136-83-6
Sample solution is provided at 25 µL, 10mM.
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TRAP-6 is a selective protease-activated receptor 1 (PAR1) agonist composed of six amino acids. TRAP-6 has a relatively simple and compact overall structure, existing as a flexible linear peptide. This structural flexibility facilitates conformational changes upon receptor binding, thereby triggering downstream signaling[1]. TRAP-6 is commonly used in research on platelet function, coagulation mechanisms, and cardiovascular diseases[2,3].
In vitro, treatment of wild-type mouse microglial cells with TRAP-6 (100, 200μM) for 24h significantly induced cell proliferation[4]. In decidual stromal cells (DSCs), TRAP-6 (100μM) treatment for 8h significantly upregulated the mRNA expression of IL-8, MCP-1, and MMP-1[5]. Pre-treatment of human washed platelets with the P2Y12 inhibitor MRS2395 (10μM) for 15min, followed by stimulation with TRAP-6 (10μM) for 30s, significantly enhanced TRAP-6-induced dense granule release, increased cytosolic Ca2+ levels, and promoted phosphorylation of GSK3β-Ser9[6].
In vivo, intraperitoneal injection of TRAP-6 (10mg/kg; three times/week) for 3 weeks in a C57BL/6→BALB/c acute graft-versus-host disease (GvHD) mouse model significantly reduced GvHD clinical scores, improved survival rates, and ameliorated histopathological damage in the colon and liver[7]. Topical application of TRAP-6 (2mM; 30μL) to skin wounds in Nembutal-anesthetized rats significantly activated mast cells in the subcutaneous adipose tissue after 3 days, resulting in a 5.4-fold decrease in heparin content within mast cells and a marked increase in degranulation and granulolysis indices[8].
References:
[1] ANDERLUH M, DOLENC M. Thrombin receptor antagonists, recent advances in PAR-1 antagonist development[J]. Current Medicinal Chemistry, 2002, 9(13): 1229-1250.
[2] WEBER M, GERDSEN F, GUTENSOHN K, et al. Enhanced platelet aggregation with TRAP-6 and collagen in platelet aggregometry in patients with venous thromboembolism[J]. Thrombosis Research, 2002, 107(6): 325-328.
[3] MÉNDEZ D, URRA F A, MILLAS-VARGAS J P, et al. Synthesis of antiplatelet ortho-carbonyl hydroquinones with differential action on platelet aggregation stimulated by collagen or TRAP-6[J]. European Journal of Medicinal Chemistry, 2020, 192: 112187.
[4] SUO Z, WU M, AMEENUDDIN S, et al. Participation of protease-activated receptor-1 in thrombin-induced microglial activation[J]. Journal of Neurochemistry, 2002, 80(4): 655-666.
[5] GOTO K, KAWANO Y, UTSUNAMIYA T, et al. Decidualization modulates a signal transduction system via protease-activated receptor-1 in endometrial stromal cells[J]. American Journal of Reproductive Immunology, 2018, 80(5): e13036.
[6] MITRUGNO A, RIGG R A, LASCHOBER N B, et al. Potentiation of TRAP-6-induced platelet dense granule release by blockade of P2Y12T activating GPR15[J]. Leukemia, 2024, 38(6): 1390-1402.
[8] UMAROVA B A, DUGINA T N, SHESTAKOVA E V, et al. Activation of rat mast cells upon stimulation of protease-activated receptor (PAR-1)[J]. Bulletin of Experimental Biology and Medicine, 2000, 129(4): 314-317.
| Cell experiment [1]: | |
Cell lines | DSCs (decidualized stromal cells) |
Preparation Method | Cultured DSCs were stimulated with 100μM TRAP-6 for 8h. Total RNA was extracted from the cells and subjected to real-time PCR to determine IL-8, MCP-1, and MMP-1 mRNA levels. |
Reaction Conditions | 100μM; 8h |
Applications | Treatment of DSCs with TRAP-6 (100μM) for 8h significantly induced the mRNA expression of IL-8, MCP-1, and MMP-1. |
| Animal experiment [2]: | |
Animal models | Murine allotransplant acute GvHD models（C57BL/6→BALB/c） |
Preparation Method | For the C57BL/6 →BALB/c model, irradiated BALB/c recipients were infused with 5 × 106 T-cell-depleted bone marrow (TCD-BM) cells and 1 × 106 T-cells from WT C57BL/6 donor. Recipient mice were intra-peritoneally injected with TRAP-6 thrice weekly for 3 weeks posttransplant. Survival and acute GvHD scores were monitored continuously. Colon and liver tissues were obtained from recipients at day 21 posttransplant. H&E staining and histological analysis were performed to assess acute GvHD features in colon and liver. |
Dosage form | 10mg/kg; three times/week; 3 weeks; i.p. |
Applications | 10mg/kg TRAP-6 decreased acute GvHD scores and increased survival of recipient mice. Histological analysis showed TRAP-6 decreased acute GvHD features in colon and liver tissues. |
References: | |
| Cas No. | 141136-83-6 | SDF | |
| Überlieferungen | PAR-1 agonist peptide; Thrombin Receptor Activator Peptide 6 | ||
| Chemical Name | (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-(diaminomethylideneamino)pentanoyl]amino]-4-oxobutanoic acid | ||
| Canonical SMILES | CC(C)CC(C(=O)NC(CC(C)C)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC(=O)N)C(=O)O)NC(=O)C(CC1=CC=CC=C1)NC(=O)C(CO)N | ||
| Formula | C34H56N10O9 | M.Wt | 748.88 |
| Löslichkeit | Soluble to 1 mg/ml in sterile water | Storage | Desiccate at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.3353 mL | 6.6766 mL | 13.3533 mL |
| 5 mM | 267.1 μL | 1.3353 mL | 2.6707 mL |
| 10 mM | 133.5 μL | 667.7 μL | 1.3353 mL |
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Quality Control & SDS
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- Purity: >99.50%
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Average Rating: 5 (Based on Reviews and 11 reference(s) in Google Scholar.)
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