1. Anti-infection Apoptosis Immunology/Inflammation NF-κB Metabolic Enzyme/Protease
  2. Antibiotic Bacterial Fungal Apoptosis Reactive Oxygen Species (ROS) TNF Receptor NO Synthase Interleukin Related NF-κB Toll-like Receptor (TLR)
  3. Papiliocin

Papiliocin 是一种兼具抗炎和抗菌活性的强效肽类抗生素。Papiliocin 主要对革兰氏阴性菌有活性。Papiliocin 对细胞具有较高的抗炎活性,通过抑制 NO 的产生以及 TNF-α 和 MIP-2 的分泌来发挥其抗炎活性。Papiliocin 通过抑制 Toll 样受体 (Toll-like Receptor) 通路和 NF-κB 参与先天防御反应机制。Papiliocin 诱导真菌 (fungal) 细胞凋亡 (apoptosis), 诱导细胞内 ROS 总水平升高。Papiliocin 在脓毒症模型中充当有效的防腐肽。Papiliocin 可用于抗炎和抗菌研究。

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Custom Peptide Synthesis

Papiliocin

Papiliocin Chemical Structure

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Papiliocin is a potent peptide antibiotic with both anti-inflammatory and antibacterial activities. Papiliocin is primarily active against Gram-negative bacteria. Papiliocin exhibits strong anti-inflammatory activity against cell, exerting its anti-inflammatory activity by inhibiting the production of NO and the secretion of TNF-α and MIP-2. Papiliocin participates in the innate defense response mechanism by inhibiting the Toll-like receptor pathway and NF-κB. Papiliocin induces apoptosis in fungal cells and increases the total level of intracellular ROS. Papiliocin acts as an effective antiseptic peptide in sepsis models. Papiliocin is useful in anti-inflammatory and antibacterial research[1][3].

IC50 & Target[1]

IL-1β

 

IL-6

 

TLR4

 

iNOS

 

体外研究
(In Vitro)

Papiliocin (37 °C 下 16 小时) 对革兰氏阴性菌 (大肠杆菌、鼠伤寒沙门氏菌和铜绿假单胞菌) 和革兰氏阳性菌 (枯草芽孢杆菌、表皮葡萄球菌和金黄色葡萄球菌) 具有抗菌活性,MIC 分别为 0.25、0.5、1、16、2、32 μM[1]
Papiliocin 对革兰氏阴性菌具有钙和镁耐受性[1]
Papiliocin (0-100 μM,37 °C 下 1 小时) 缺乏溶血活性,对 RAW264.7 细胞无细胞毒性,IC50 为 58 μm[1]
Papiliocin (0-25 μM,3-24 小时) 可抑制 LPS (HY-D1056) 刺激的 RAW264.7 细胞中 NO、TNF-α、MIP-2、iNOS、TLR4、NF-κB 以及所有炎症细胞因子 IL-1β、IL-6、MIP-1、MIP-2 和 TNF-α 基因的表达[1]
Papiliocin (0-10 μM) 可诱导脂质囊泡通透性,在胶束或 SUV 中表现出较低的 Stern-Volmer 猝灭常数 (KSV),并通过与 LPS 聚集体的相互作用导致 LPS 聚集体的解离[1]
Papiliocin (30 μM,28 °C,2 小时) 可诱导白色念珠菌细胞中 ROS 的产生,并增加细胞内羟基自由基水平[2]
Papiliocin (30 μM,28 °C,2 小时) 可诱导白色念珠菌细胞中细胞凋亡、膜去极化和间质胱天蛋白酶活化,以及 DNA 损伤[2]
Papiliocin (0-50 μM) 可取代 LPS 上 74.6% 的 BC 探针,并中和 LPS,结合亲和力为 0.063 μM[3]
Papiliocin (40 μM,30 分钟) 可抑制 52% 的 FITC-LPS 与 RAW 264.7 细胞表面的结合,同时竞争性地取代 RAW 264.7 细胞上 LPS-受体复合物上 25% 的预结合 LPS[3]
Papiliocin (0-100 μM) 可降低 TLR4 介导的 SEAP 活性,IC50 为 1.1 μM[3]
Papiliocin (0.1-10 μM,1 小时) 可阻断 LPS 诱导的炎症通过靶向 TLR4 和 MAPK 通路以及阻断 RAW 264.7 细胞中的 p-NF-κB 核易位来产生级联[3]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

ELISA Assay[1]

Cell Line: LPS (20 ng/mL)-stimulated RAW264.7 cells
Concentration: 1, 10 μM
Incubation Time: 18  h
Result: Inhibited the production of TNF-α and MIP-2.

RT-PCR[1]

Cell Line: LPS (20 ng/mL)-stimulated RAW264.7 cells
Concentration: 20 μM
Incubation Time: 3  h
Result: Inhibited the expression of iNOS and all inflammatory cytokines, including IL-1β, IL-6, MIP-1, MIP-2, and TNF-α.

Western Blot Analysis[1]

Cell Line: LPS (20 ng/mL)-stimulated RAW264.7 cells
Concentration: 25 μM
Incubation Time: 24  h
Result: Inhibited TLR4 and NF-κB expression and prevented the translocation of NF-κB from the cytoplasm to the nucleus.

Apoptosis Analysis[2]

Cell Line: Candida albicans cells
Concentration: 30 μM
Incubation Time: 28 °C for 2 h
Result: Induced apoptosis cell death, with the early apoptotic cells of 61.14%, the late apoptotic of 0.52%.
Induced the breakdown of ΔΨm and the loss of mitochondrial permeability.
Induced the generation of strong oxidant hydroxyl radicals.
Increased the proportion of TUNEL-positive cell nuclei.

Western Blot Analysis[3]

Cell Line: LPS (50 ng/mL)-stimulated RAW264.7 cells
Concentration: 0.1, 0.5, 1 μM
Incubation Time: 1  h
Result: Reduced MyD88 overexpression and phosphorylation levels of TAK1, p38, c-Jun N-terminal kinase (JNK), and extracellular signal-regulated kinase (ERK).

Immunofluorescence[3]

Cell Line: LPS (50 ng/mL)-stimulated RAW264.7 cells
Concentration: 10 μM
Incubation Time: 1  h
Result: Reduced expression of Alexa 546 inhibited Lp-NF-κB p65 translocation.
分子量

4002.80

Formula

C183H314N56O44

Sequence

Arg-Trp-Lys-Ile-Phe-Lys-Lys-Ile-Glu-Lys-Val-Gly-Arg-Asn-Val-Arg-Asp-Gly-Ile-Ile-Lys-Ala-Gly-Pro-Ala-Val-Ala-Val-Val-Gly-Gln-Ala-Ala-Thr-Val-Val-Lys-NH2

Sequence Shortening

RWKIFKKIEKVGRNVRDGIIKAGPAVAVVGQAATVVK-NH2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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