2. Immunology/Inflammation Anti-infection
  3. Toll-like Receptor (TLR) Bacterial
  4. Pap12-6-10

Pap12-6-10 是一种 MD-2 配体，能结合 MD-2 疏水口袋抑制 TLR4/MD-2 复合物二聚化与下游炎性信号传导，还可结合 LPS 通透细菌细胞膜、诱导氧化应激致细菌死亡。Pap12-6-10 能通过 TLR4 信号通路调控 LPS 诱导的炎性反应，对多重耐药革兰氏阴性菌有抗菌活性。Pap12-6-10 的耐药性产生倾向及临床前细胞毒性均较低，还可在脓毒症小鼠模型中预防器官损伤。Pap12-6-10 可用于革兰氏阴性脓毒症、耐碳青霉烯类鲍曼不动杆菌感染的相关研究。

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Custom Peptide Synthesis

Pap12-6-10

Pap12-6-10 Chemical Structure

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Pap12-6-10 相关抗体

Top Publications Citing Use of Products

查看 Toll-like Receptor (TLR) 亚型特异性产品:

查看所有亚型
TLR3 TLR8 TLR9 TLR2 TLR4 TLR7 TLR1 TLR6

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Pap12-6-10 is an MD-2 ligand that binds to the hydrophobic pocket of MD-2 to inhibit the dimerization of the TLR4/MD-2 complex and downstream inflammatory signal transduction. Pap12-6-10 also binds to LPS to permeabilize bacterial cell membranes and induce oxidative stress, leading to bacterial death. Pap12-6-10 regulates LPS-induced inflammatory responses through the TLR4 signaling pathway and exhibits antibacterial activity against multidrug-resistant Gram-negative bacteria. Pap12-6-10 shows low tendency to induce drug resistance and low preclinical cytotoxicity, and it prevents organ damage in a mouse model of sepsis. Pap12-6-10 can be used for research related to Gram-negative sepsis and carbapenem-resistant Acinetobacter baumannii infections[1].
IC50 & Target

TLR4

 

体外研究
(In Vitro)

Pap12-6-10 (10 μM；预处理 30 分钟，随后 LPS 处理孵育 30 分钟) 可抑制 Alexa Fluor 488 偶联的 LPS (3 μg/mL) 与 RAW 264.7 细胞表面受体的结合[1]。

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

Pap12-6-10 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route Cmax Tmax T1/2
Rat[1] 2 mg/kg i.v. 4461.134 ng/mL 0.25 h 1.819 h
体内研究
(In Vivo)

Pap12-6-10 (1 mg/kg; i.p.; 于E. coli K1 感染前 1 小时单次给药) 在E. coli K1 诱导的脓毒症模型中表现出强效的体内抗菌与抗炎活性，可提高生存率并减轻器官损伤[1]。
Pap12-6-10 (腹腔注射；每 4 小时 1 次；共 12 小时) 在CRAB诱导的脓毒症中表现出强大的抗菌作用，可提高存活率并降低细菌载量与炎症反应[1]。

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

Animal Model: ICR mice (female, 6 weeks old)[1]
Dosage: 1 mg/kg
Administration: i.p.; single dose (1 hour before E. coli K1 infection)
Result: Reduced bacterial counts in the lung (>49.0%), liver (>76.2%), and kidneys (>53.3%); decreased endotoxin levels by over 60.4%; suppressed pro-inflammatory cytokine levels (TNF-α by 47.3%, IL-6 by 36.5%, IL-1β by 54.6%); reduced AST, ALT, and BUN levels by 46.5%, 55.3%, and 49.9% respectively; improved survival rate to 50% at 96 hours post-infection.
分子量

1631.06

Formula

C82H131N23O12
Sequence

{d-Arg}-{d-Trp}-{d-Lys}-{d-Ala}-{d-Phe}-{d-Lys}-{d-Lys}-{d-Leu}-{d-Leu}-{d-Lys}-{d-Lys}-{d-Trp}-NH2
Sequence Shortening

rwkafkkllkkw-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

Pap12-6-10 相关分类

  • 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.

Keywords:

Pap12-6-10Toll-like Receptor (TLR)BacterialRAW 264.7 cellE. coli K1sepsis mouse modelsMD-2TLR4/MD-2 complexcarbapenem-resistant Acinetobacter baumanniiTLR4 signaling pathwaysgram-negative sepsismultidrug-resistant Gram-negative bacteriaLPSInhibitorinhibitorinhibit

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