Quinupristin-Dalfopristin Mesylate

Quinupristin-Dalfopristin Mesylate

Catalog Number:
M001342209TOK
Mfr. No.:
TOK-Q009
Price:
$320
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      • Overview
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          Background

          While both dalfopristin and quinupristin have bacteriostatic effects, they act synergistically to kill gram-positive bacteria, as well as some gram-negative and anaerobic bacteria. Dalfopristin binds to the 23s portion of the 50s ribosomal subnit and inhibits peptidyl transfer, as well as changing conformation to enhance binding of quinupristin. Quinupristin binds to a nearby site on the 50s ribosomal subunit and prevent elongation of the polypeptide as well as incomple polypeptide chains to be released prematurely.

      • Properties
        • CAS Number
          126602-89-9
          Molecular Formula
          C54H71N9O13S2 (for quinupristin mesylate); C35H54N4O12S2 (for dalfopristin mesylate)
          Molecular Weight
          1118.3 (for quinupristin mesylate) ; 786.9 (for dalfopristin mesylate)
          Appearance
          White to light-yellow solid
          Storage
          -20°C

          * For research use only

      • Applications
        • Application Description
          Spectrum: Quinupristin/dalfopristin is active against a range of gram-positive bacteria including meticillin- and multidrug-resistant strains of Staphylococcus aureus and S. epidermidis, vancomycin-resistant Enterococcus faecium (but not E. faecalis), and penicillin- and macrolide-resistant Streptococcus pneumoniae. It is also active against the anaerobe Clostridium perfringens, and Gram-negative bacteria Legionella pneumophila, Moraxella catarrhalis (Branhamella catarrhalis), Mycoplasma pneumoniae, and Neisseria meningitidis

          Microbiology Applications: Quinupristin/dalfopristin received approval for use in adults for the treatment of infections caused by susceptible strains of vancomycin-resistant Enterococcus faecium(VREF) and for the treatment of complicated skin and skin structure infections caused by Staphylococcus aureus (methicillin-susceptible) or Streptococcus pyogenes

          Eukaryotic Cell Culture Applications: In vitro drug interaction studies have shown that Synercid (Quinupristin/dalfopristin) significantly inhibits cytochrome P450 3A4. Synercid has been shown to be a major inhibitor (in vitro inhibits 70% cyclosporin A biotransformation at 10 mcg/mL of Synercid) of the activity of cytochrome P450 3A4 isoenzyme.The Pip/ptr promoter complex was dissociated by pristinamycin I but not by any of the other non-streptogramin antibiotics. These prokaryotic regulatory elements served as the basis for the development of systems allowing repression or induction of cloned genes in mammalian and plant cells in response to streptogramin antibiotics including pristinamycin, virginiamycin, and Synercid.

          Cancer Applications: In cancer patients, quinupristin-dalfopristin treatment is associated with a relatively high frequency of myalgias/arthralgias; however, profound thrombocytopenia might limit the choice of linezolid in a subpopulation of cancer patients

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