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.
For research use only. We do not sell to patients.
- Formula: C82H131N23O12
- Molecular Weight:1631.06
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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TLR4 |
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.
| Species | Dose | Route | Cmax | Tmax | T1/2 |
|---|---|---|---|---|---|
| Rat[1] | 2 mg/kg | i.v. | 4461.134 ng/mL | 0.25 h | 1.819 h |
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.
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Animal Model:ICR mice (female, 6 weeks old)[1]
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Dosage:1 mg/kg
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Administration:i.p.; single dose (1 hour before E. coli K1 infection)
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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.
Chemical Information
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Molecular Weight 1631.06
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Formula C82H131N23O12
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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
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Sequence Shortening
rwkafkkllkkw-NH2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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