PAR-4 Agonist Peptide, amide TFA (PAR-4-AP (TFA)) (Synonyms: PAR-4-AP TFA; AY-NH2 TFA) |
| Katalog-Nr.GC33599 |
PAR-4-Agonist-Peptid, Amid TFA (PAR-4-AP (TFA)) (PAR-4-AP TFA; AY-NH2 TFA) ist ein Proteinase-aktivierter Rezeptor-4 (PAR-4)-Agonist, der keine Wirkung hat auf entweder PAR-1 oder PAR-2 und deren Wirkungen durch einen PAR-4-Antagonisten blockiert werden.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1228078-65-6
Sample solution is provided at 25 µL, 10mM.
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PAR-4 agonist peptide, amide TFA (PAR-4-AP (TFA)) is a synthetic peptide primarily used to activate protease-activated receptor 4 (PAR-4) [1]. PAR-4 is a G protein-coupled receptor widely expressed in platelets and other cell types, playing a role in regulating various physiological and pathological processes, including blood coagulation and inflammatory responses [2].
PAR-4 agonist peptide, amide TFA (PAR-4-AP (TFA))(100μM；1-24h) exerts a potential tumor suppressor effect in esophageal squamous cell carcinoma (ESCC) by activating the PAR4 receptor, which inhibits the expression of DNA methyltransferase 1 (DNMT1) and histone deacetylase 2 (HDAC2), while increasing the expression of the tumor suppressor p16 [3]. PAR-4 agonist peptide, amide TFA (PAR-4-AP (TFA)) (30μM；1-24h) inhibits phagocytosis in mouse macrophages and enhances the production of nitric oxide (NO) and reactive oxygen species (ROS), modulating the expression of inflammatory factors and the transcriptional activity of NF-κB [4].
PAR-4 agonist peptide, amide TFA (PAR-4-AP (TFA)) effectively induced sustained bladder hypersensitivity [5-6]. PAR-4 Agonist Peptide, amide TFA (PAR-4-AP (TFA))(100μg; Intracolonic administration) inhibits the inflammatory response in a rat model by downregulating inflammatory mediators in mast cells through the MAPK signaling pathway[7].
References:
[1] Hollenberg MD, Compton SJ. International Union of Pharmacology. XXVIII. Proteinase-activated receptors. Pharmacol Rev. 2002 Jun;54(2):203-17. doi: 10.1124/pr.54.2.203. PMID: 12037136.
[2] Han X, Nieman MT. PAR4 (Protease-Activated Receptor 4): PARticularly Important 4 Antiplatelet Therapy. Arterioscler Thromb Vasc Biol. 2018 Feb;38(2):287-289. doi: 10.1161/ATVBAHA.117.310550. PMID: 29367229; PMCID: PMC5788293.
[3] Wang M, An S, Wang D, Ji H, Guo X, Wang Z. Activation of PAR4 Upregulates p16 through Inhibition of DNMT1 and HDAC2 Expression via MAPK Signals in Esophageal Squamous Cell Carcinoma Cells. J Immunol Res. 2018 Sep 30;2018:4735752. doi: 10.1155/2018/4735752. PMID: 30363984; PMCID: PMC6186345.
[4] Barra A, Freitas KM, Marconato DG, Faria-Pinto P, Lopes MTP, Klein A. Protease-activated receptor 4 plays a role in lipopolysaccharide-induced inflammatory mechanisms in murine macrophages. Naunyn Schmiedebergs Arch Pharmacol. 2021 May;394(5):853-862. doi: 10.1007/s00210-020-02014-w. Epub 2020 Nov 7. PMID: 33159803.
[5] Ye S, Agalave NM, Ma F, D Mahmood DF, Al-Grety A, Khoonsari PE, Svensson CI, Kultima K, Vera PL. Lumbosacral spinal proteomic changes during PAR4-induced persistent bladder pain. Neurosci Lett. 2024 Jan 1;818:137563. doi: 10.1016/j.neulet.2023.137563. Epub 2023 Nov 28. PMID: 38036085; PMCID: PMC10929774.
[6] Kouzoukas DE, Ma F, Meyer-Siegler KL, Westlund KN, Hunt DE, Vera PL. Protease-Activated Receptor 4 Induces Bladder Pain through High Mobility Group Box-1. PLoS One. 2016 Mar 24;11(3):e0152055. doi: 10.1371/journal.pone.0152055. PMID: 27010488; PMCID: PMC4806866.
[7] Hao Y, Niu H, An S, Wang M, Wang Z. Downregulation of iNOS, IL-1β, and P2X7 Expression in Mast Cells via Activation of PAR4 Contributes to the Inhibition of Visceral Hyperalgesia in Rats. J Immunol Res. 2018 May 9;2018:3256908. doi: 10.1155/2018/3256908. PMID: 29854833; PMCID: PMC5966670.
| Cell experiment [1]: | |
Cell lines | HUVECs/HASMCs |
Preparation Method | Human umbilical vein endothelial cells (HUVECs) or human aortic smooth muscle cells (HASMCs) were cultured in DMEM medium containing 10% fetal bovine serum and 1% penicillin-streptomycin until reaching 70-80% confluence. Prior to the addition of non-lipid tissue factor and Ca²⁺, PAR-4 Agonist Peptide, amide TFA (PAR-4-AP (TFA)) was added to the cells and incubated for 15 minutes for pre-treatment. Subsequently, non-lipid tissue factor and Ca²⁺ were added to the cells after pre-treatment to induce thrombin generation, with the reaction conditions set at 37°C. Samples were collected at different time points to monitor thrombin generation. |
Reaction Conditions | 200µmol/L ; 15mins |
Applications | The PAR-4 agonist peptide, amide TFA (PAR-4-AP (TFA)), accelerates thrombin generation and significantly shortens the time to reach half-peak thrombin levels during tissue factor-induced coagulation, thereby enhancing the coagulation response. |
| Animal experiment [2]: | |
Animal models | C57BL/6(bladder hyperalgesia model) |
Preparation Method | The mice were anesthetized using isoflurane (3% for induction and 1.5% for maintenance) and were transurethrally catheterized with a PE10 catheter (11mm in length). To prepare for the intravesical instillation, urine was drained by gently applying pressure to the lower abdomen. The treatment involved instilling 100 µL of PAR-4 agonist peptide, amide TFA (PAR-4-AP (TFA))(100µM in sterile PBS, pH 7.4) into the bladder. The control group received an equivalent volume of scrambled peptide (YAPGKP-NH2, 100µM in sterile PBS). |
Dosage form | The PAR-4 agonist peptide, amide TFA (PAR-4-AP (TFA)) (100µM), was administered via intravesical injection three times at 48-hour intervals, with remained in the bladderfor 1 h. |
Applications | PAR-4 agonist peptide, amide TFA (PAR-4-AP (TFA)), effectively induced sustained bladder hypersensitivity in a mouse model. |
References: | |
| Cas No. | 1228078-65-6 | SDF | |
| Überlieferungen | PAR-4-AP TFA; AY-NH2 TFA | ||
| Canonical SMILES | Ala-Tyr-Pro-Gly-Lys-Phe-NH2 | ||
| Formula | C36H49F3N8O9 | M.Wt | 794.82 |
| Löslichkeit | DMSO : ≥ 250 mg/mL (314.54 mM) | Storage | Store 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 | 1.2581 mL | 6.2907 mL | 12.5815 mL |
| 5 mM | 251.6 μL | 1.2581 mL | 2.5163 mL |
| 10 mM | 125.8 μL | 629.1 μL | 1.2581 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 24 reference(s) in Google Scholar.)
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