PAβN dihydrochloride

CAS No. 100929-99-5

PAβN dihydrochloride( MC-207,110 dihydrochloride,Phe-Arg-β-naphthylamide dihydrochloride )

Catalog No. M22016 CAS No. 100929-99-5

PAβN dihydrochloride is an inhibitor of efflux pump. PAβN reduces the MICs in nine ciprofloxacin-resistant isolates, and in four of these, PAβN increases the susceptibility by twofold.?

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    PAβN dihydrochloride
  • Note
    Research use only, not for human use.
  • Brief Description
    PAβN dihydrochloride is an inhibitor of efflux pump. PAβN reduces the MICs in nine ciprofloxacin-resistant isolates, and in four of these, PAβN increases the susceptibility by twofold.?
  • Description
    PAβN dihydrochloride is an inhibitor of efflux pump. PAβN reduces the MICs in nine ciprofloxacin-resistant isolates, and in four of these, PAβN increases the susceptibility by twofold.?Moreover, PAβN restores ciprofloxacin susceptibility in five of the ciprofloxacin-resistant isolates.?In addition, clear effects of NMP on the ciprofloxacin MICs are seen for 20 of these ciprofloxacin-resistant isolates.
  • In Vitro
    PAβN increases the susceptibilities of the three pump-overexpressing mutants of P. aeruginosa to levofloxacin 64-fold. PAβN also potentiates the activity of levofloxacin against strain PAM2391 containing plasmid pAGH97 with the mexXY genes and against wild-type strain PAM1020. PAβN has an effect on susceptibilities to other antibiotics that are substrates of efflux pumps. PAβN increases levels of accumulation of efflux pump substrates inside the cell. It enhances the activity of levofloxacin against clinical isolates of P. aeruginosa. PAβN reduces the MICs in nine ciprofloxacin-resistant isolates, and in four of these, PAβN increases the susceptibility by twofold. Moreover, PAβN restores ciprofloxacin susceptibility in five of the ciprofloxacin-resistant isolates. In addition, clear effects of NMP on the ciprofloxacin MICs are seen for 20 of these ciprofloxacin-resistant isolates. PAβN permeabilizes bacterial membranes in a concentration-dependent manner at levels below those typically used in combination studies, and this additional mode of action should be considered when using PAβN as a control for efflux studies.
  • In Vivo
    ——
  • Synonyms
    MC-207,110 dihydrochloride,Phe-Arg-β-naphthylamide dihydrochloride
  • Pathway
    GPCR/G Protein
  • Target
    Antibacterial
  • Recptor
    Bacterial| efflux pump
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    100929-99-5
  • Formula Weight
    519.47
  • Molecular Formula
    C25H32Cl2N6O2
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO:95mg/ml (182.88 Mm);H2O:14.29 mg/mL (27.51 mM; Need ultrasonic)
  • SMILES
    Cl.Cl.N[C@@H](CC1=CC=CC=C1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)NC1=CC2=CC=CC=C2C=C1
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Lomovskaya O, et al. Identification and characterization of inhibitors of multidrug resistance efflux pumps in Pseudomonas aeruginosa: novel agents for combination therapy. Antimicrob Agents Chemother. 2001 Jan;45(1):105-16.
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