PAR-4 Agonist Peptide, amide TFA (PAR-4-AP (TFA))
(Synonyms: PAR-4-AP TFA; AY-NH2 TFA) 目录号 : GC33599
PAR-4 Agonist Peptide, amide TFA (PAR-4-AP (TFA)) 是一种合成肽，主要用于激活蛋白酶激活受体4（PAR-4）。
Cas No.:1228078-65-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| 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: | |
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.
PAR-4 Agonist Peptide, amide TFA (PAR-4-AP (TFA)) 是一种合成肽，主要用于激活蛋白酶激活受体4（PAR-4）[1]。PAR-4是一种G蛋白偶联受体，广泛表达于血小板和其他细胞类型中，参与调节多种生理和病理过程，包括血液凝固、炎症反应[2]。
PAR-4 Agonist Peptide, amide TFA (PAR-4-AP (TFA)) (100μM；1-24h)通过激活PAR4受体，抑制DNA甲基转移酶1（DNMT1）和组蛋白去乙酰化酶2（HDAC2）的表达，增加肿瘤抑制因子p16的表达，从而在食管鳞状细胞癌（ESCC）中发挥潜在的肿瘤抑制作用[3]。PAR-4 Agonist Peptide, amide TFA (PAR-4-AP (TFA)) (30μM；1-24h)通过激活PAR4受体，抑制小鼠巨噬细胞的吞噬作用，同时增强一氧化氮（NO）和活性氧（ROS）的产生，调节炎症因子和NF-κB的转录活性[4]。
PAR-4 Agonist Peptide, amide TFA (PAR-4-AP (TFA)) 在小鼠模型中有效诱导了持续膀胱超敏感[5-6]。PAR-4 Agonist Peptide, amide TFA (PAR-4-AP (TFA))(100μg; Intracolonic administration)在大鼠模型中通过下调肥大细胞中的炎症介质，通过MAPK信号通路抑制炎症反应[7]。
| Cas No. | 1228078-65-6 | SDF | |
| 别名 | PAR-4-AP TFA; AY-NH2 TFA | ||
| Canonical SMILES | Ala-Tyr-Pro-Gly-Lys-Phe-NH2 | ||
| 分子式 | C36H49F3N8O9 | 分子量 | 794.82 |
| 溶解度 | DMSO : ≥ 250 mg/mL (314.54 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.2581 mL | 6.2907 mL | 12.5815 mL |
| 5 mM | 0.2516 mL | 1.2581 mL | 2.5163 mL |
| 10 mM | 0.1258 mL | 0.6291 mL | 1.2581 mL |
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动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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