1. Anti-infection
  2. Bacterial Antibiotic
  3. Murepavadin

Murepavadin (POL7080), a 14-amino-acid cyclic peptide, is a highly potent, specific antibiotic. Murepavadin exhibits a potent antimicrobial activity for P. aeruginosa with both MIC50 and MIC90 values of 0.12 mg/L. Murepavadin also can target the lipopolysaccharide transport portin D. Murepavadin can be used for the research of bacterial resistance.

For research use only. We do not sell to patients.

Custom Peptide Synthesis

Murepavadin Chemical Structure

Murepavadin Chemical Structure

CAS No. : 944252-63-5

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Description

Murepavadin (POL7080), a 14-amino-acid cyclic peptide, is a highly potent, specific antibiotic. Murepavadin exhibits a potent antimicrobial activity for P. aeruginosa with both MIC50 and MIC90 values of 0.12 mg/L. Murepavadin also can target the lipopolysaccharide transport portin D. Murepavadin can be used for the research of bacterial resistance[1][2].

IC50 & Target

MIC50: 0.12 mg/L(P. aeruginosa)[2] MIC90: 0.12 mg/L(P. aeruginosa)[2] IC50: 5.84 μM (gentamicin)[2]

In Vitro

Murepavadin has activity against P. aeruginosa with MIC50 and MIC90 values both of 0.12 mg/L[2].
Murepavadin inhibits megalin-mediated uptake of gentamicin in vitro with an IC50 value of 5.84 μM[2].

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

In Vivo

Murepavadin (s.c.; 0-100 mg/kg) is active in pre-clinical animal models including infections with XDR isolates[2].

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

Animal Model: murine models of P. aeruginosa infection[2]
Dosage: 0-100 mg/kg
Administration: Subcutaneous, q24h or q12h
Result: Resulted in an increase in survival rate to 100% and showed significantly lower CFU levels both in the blood and in the peritoneal fluid at 2 and 10 mg/kg 1 h post-infection.
Animal Model: Mouse, rat, rabbit, and monkey[2]
Dosage: 0-5 mg/kg
Administration: Intraperitoneal or subcutaneous, single
Result: Followed a two-compartment model following intravenous administration and decline of plasma concentrations.
Distributed into the aqueous phase of the body, and systemic plasma clearance (CL) values were similar to the species-specific glomerular filtration rates (GFRs) .
Had high bioavailability (67.79%) after subcutaneous (s.c.) administration in rats but had low oral bioavailability (<0.01%).
Had a linear relationship between ELF AUC and unbound plasma AUC in mouse.
Did not readily cross the blood/brain barrier.
Clinical Trial
Molecular Weight

1553.81

Formula

C73H112N22O16

CAS No.
Sequence

Cyclo(Ala-Ser-{d-Pro}-Pro-Thr-Trp-Ile-{Dab}-{Orn}-{d-Dab}-{Dab}-Trp-{Dab}-{Dab})

Sequence Shortening

Cyclo(AS-{d-Pro}-PTWI-{Dab}-{Orn}-{d-Dab}-{Dab}-W-{Dab}-{Dab})

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility
In Vitro: 

H2O

Peptide Solubility and Storage Guidelines:

1.  Calculate the length of the peptide.

2.  Calculate the overall charge of the entire peptide according to the following table:

  Contents Assign value
Acidic amino acid Asp (D), Glu (E), and the C-terminal -COOH. -1
Basic amino acid Arg (R), Lys (K), His (H), and the N-terminal -NH2 +1
Neutral amino acid Gly (G), Ala (A), Leu (L), Ile (I), Val (V), Cys (C), Met (M), Thr (T), Ser (S), Phe (F), Tyr (Y), Trp (W), Pro (P), Asn (N), Gln (Q) 0

3.  Recommended solution:

Overall charge of peptide Details
Negative (<0) 1.  Try to dissolve the peptide in water first.
2.  If water fails, add NH4OH (<50 μL).
3.  If the peptide still does not dissolve, add DMSO (50-100 μL) to solubilize the peptide.
Positive (>0) 1.  Try to dissolve the peptide in water first.
2.  If water fails, try dissolving the peptide in a 10%-30% acetic acid solution.
3.  If the peptide still does not dissolve, try dissolving the peptide in a small amount of DMSO.
Zero (=0) 1.  Try to dissolve the peptide in organic solvent (acetonitrile, methanol, etc.) first.
2.  For very hydrophobic peptides, try dissolving the peptide in a small amount of DMSO, and then dilute the solution with water to the desired concentration.
Purity & Documentation
References
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Murepavadin Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (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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Murepavadin
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HY-P1674
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