PBP 10
(Synonyms: 甲酰肽受体2(FPR2)拮抗剂多肽) 目录号 : GC17409
PBP 10是一种具有细胞通透性的甲酰肽受体2（FPR2）拮抗剂。
Cas No.:794466-43-6
Sample solution is provided at 25 µL, 10mM.
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PBP 10 is a cell-permeable formyl peptide receptor 2 (FPR2) antagonist[1-2]. PBP 10 exhibits multiple biological activities, including antibacterial, antiviral, and cancer-inhibitory effects[3-4].
In vitro, pretreatment of human keratinocytes (HaCaT) with PBP 10 (2-10μg/mL) for 20 minutes significantly suppresses the release of pro-inflammatory mediators such as nitric oxide (NO), reactive oxygen species (ROS), and interleukin-8 (IL-8) induced by stimulation with lipopolysaccharide (LPS; 1μg/mL) or lipoteichoic acid (LTA; 1μg/mL), while also reversing inflammation-related nanomechanical changes, such as the reduction in cell stiffness caused by LPS[5]. Pretreatment of RT4 Schwann cells with PBP 10 (1 μM) for 20 minutes, followed by stimulation with fMLF (10nM–100nM) for 6 hours, significantly inhibits fMLF-induced upregulation of Fpr2 protein expression and the decrease in p-NFκB levels, while also reversing changes in the expression of CCR2, CXCR4, and PKCβ[6].
References:
[1] Forsman H, Andréasson E, Karlsson J, et al. Structural characterization and inhibitory profile of formyl peptide receptor 2 selective peptides descending from a PIP2-binding domain of gelsolin. J Immunol. 2012 Jul 15;189(2):629-37.
[2] Holdfeldt A, Winther M, Gabl M, et al. Data on human neutrophil activation induced by pepducins with amino acid sequences derived from β2AR and CXCR4. Data Brief. 2016 Jun 1;8:411-4.
[3] Courtin N, Fotso AF, Fautrad P, et al. Antiviral activity of formyl peptide receptor 2 antagonists against influenza viruses. Antiviral Res. 2017 Jul;143:252-261.
[4] Jia G, Wang X, Wu W, et al. LXA4 enhances prostate cancer progression by facilitating M2 macrophage polarization via inhibition of METTL3. Int Immunopharmacol. 2022 Jun;107:108586.
[5] Korimová A, Dubový P. N-Formylated Peptide Induces Increased Expression of Both Formyl Peptide Receptor 2 (Fpr2) and Toll-Like Receptor 9 (TLR9) in Schwannoma Cells-An In Vitro Model for Early Inflammatory Profiling of Schwann Cells. Cells. 2020 Dec 11;9(12):2661.
[6] Xu J, Su Z, Cheng X, et al. High PPT1 expression predicts poor clinical outcome and PPT1 inhibitor DC661 enhances sorafenib sensitivity in hepatocellular carcinoma. Cancer Cell Int. 2022 Mar 11;22(1):115.
PBP 10是一种具有细胞通透性的甲酰肽受体2（FPR2）拮抗剂[1-2]。PBP 10具有多种生物学活性，包括抗菌、抗病毒和抑制癌症[3-4]。
在体外，PBP 10（2-10μg/mL）预处理人皮肤角质形成细胞（HaCaT）孵育20分钟，可显著抑制由脂多糖（LPS；1μg/mL）或脂磷壁酸（LTA；1μg/mL）刺激所诱导的一氧化氮（NO）、活性氧（ROS）及白细胞介素-8（IL-8）等促炎介质的释放，同时逆转LPS引起的细胞刚度降低等炎症反应相关的纳米力学特性改变[5]。PBP 10（1μM）预处理RT4 Schwann细胞20分钟，随后以fMLF（10nM–100nM）刺激6小时，显著抑制fMLF诱导的Fpr2蛋白表达上调和p-NFκB水平降低，同时逆转CCR2、CXCR4及PKCβ的表达变化[6]。
| Cell experiment [1]: | |
Cell lines | HaCaT cells (human immortalized keratinocyte cell line) |
Preparation Method | HaCaT cells were maintained in high-glucose Dulbecco’s Modified Eagle Medium (DMEM) supplemented with 10% fetal bovine serum (FBS), 2mM L-glutamine, and antibiotics (50U/mL penicillin, 50µg/mL streptomycin) at 37°C, 5% CO₂. Cells were pretreated with PBP 10 (2–10µg/mL) for 20 min, followed by stimulation with bacterial lipopolysaccharide (LPS; 1µg/mL) or lipoteichoic acid (LTA; 1µg/mL) for 24h in serum-free conditions. |
Reaction Conditions | 2–10µg/mL; pretreatment for 20min |
Applications | PBP 10 significantly suppressed LPS/LTA-induced production of inflammatory mediators, including nitric oxide (NO), reactive oxygen species (ROS), and interleukin-8 (IL-8), in a dose-dependent manner. PBP 10 also reversed LPS-induced softening of cell stiffness, as measured by atomic force microscopy (AFM), indicating restoration of cytoskeletal integrity. |
References: | |
| Cas No. | 794466-43-6 | SDF | |
| 别名 | 甲酰肽受体2(FPR2)拮抗剂多肽 | ||
| 化学名 | (1E,3S,4Z,6S,7Z,9S,10Z,12S,13Z,15S,16Z,18S,19Z,21S,22Z,25Z,27S,28Z,30S)-21-(4-aminobutyl)-12-benzyl-1-(2-(3,6-bis(diethylamino)xanthylium-9-yl)phenyl)-6,27,30-tris(3-guanidinopropyl)-1,4,7,10,13,16,19,22,25,28-decahydroxy-3,15-bis(3-hydroxy-3-iminopropyl) | ||
| Canonical SMILES | CCN(C(C=CC1=C2C3=CC=CC=C3/C(O)=N\[C@@](/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/C/C(O)=N/[C@@](/C(O)=N/[C@@](C([O-])=O)([H])CCCNC(N)=N)([H])CCCNC(N)=N)([H])CCCCN)([H])C(C)C)([H])CCC(O)=N)([H])CC4=CC=CC=C4 | ||
| 分子式 | C84H126N24O15 | 分子量 | 1712.1 |
| 溶解度 | Soluble to 2 mg/ml in Water | 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 | 584.1 μL | 2.9204 mL | 5.8408 mL |
| 5 mM | 116.8 μL | 584.1 μL | 1.1682 mL |
| 10 mM | 58.4 μL | 292 μL | 584.1 μL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet