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

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.

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Pap12-6-10

Pap12-6-10 Chemical Structure

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Pap12-6-10 Related Antibodies

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Description

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

 

In Vitro

Pap12-6-10 (10 μM; 30 min pretreatment, 30 min LPS exposure incubation) inhibits binding of Alexa Fluor 488-conjugated LPS (3 μg/mL) to RAW 264.7 cell surface receptors[1].

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

Pap12-6-10 Related Antibodies
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
In Vivo

Pap12-6-10 (1 mg/kg; i.p.; single dose 1 hour before E. coli K1 infection) exhibits potent in vivo antibacterial and anti-inflammatory activity in E. coli K1-induced sepsis, improving survival and reducing organ damage[1].
Pap12-6-10 (i.p.; every 4 hours; 12 hours) demonstrates strong antiseptic effects in CRAB-induced sepsis, enhancing survival and reducing bacterial burden and inflammation[1].

MedChemExpress (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.
Molecular Weight

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Pap12-6-10 Related Classifications

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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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