Polymyxin B1 -d 7 TFA is the deuterium labeled Polymyxin B1 TFA. Polymyxin B1 is a potent antimicrobial lipopeptide first derived from Bacilus polymyxa. Polymyxin B1 is the major component in Polymyxin B. Polymyxin B1 can induce lysis of bacterial cells through interaction with their membranes. Polymyxin B1 has the potential for multidrug-resistant Gram-negative bacterial infections treatment [1] [2].
In Vitro, Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs.
References:
[1]. Kwa AL, et al. Pharmacokinetics of polymyxin B1 in patients with multidrug-resistant Gram-negative bacterial infections. Diagn Microbiol Infect Dis. 2008 Feb;60(2):163-7.
[2]. Berglund NA, et al. Interaction of the antimicrobial peptide polymyxin B1 with both membranes of E. coli: a molecular dynamics study. PLoS Comput Biol. 2015 Apr 17;11(4):e1004180.
[3]. Tam VH, et al. In vitro potency of various polymyxin B components. Antimicrob Agents Chemother. 2011 Sep;55(9):4490-1.
[4]. Alonso MA, et al. Compounds affecting membranes that inhibit protein synthesis in yeast. Antimicrob Agents Chemother. 1979 Dec;16(6):750-6.
[5]. Sivanesan S, et al. Pharmacokinetics of the Individual Major Components of Polymyxin B and Colistin in Rats. J Nat Prod. 2017 Jan 27;80(1):225-229.
In Vitro, Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs.
References:
[1]. Kwa AL, et al. Pharmacokinetics of polymyxin B1 in patients with multidrug-resistant Gram-negative bacterial infections. Diagn Microbiol Infect Dis. 2008 Feb;60(2):163-7.
[2]. Berglund NA, et al. Interaction of the antimicrobial peptide polymyxin B1 with both membranes of E. coli: a molecular dynamics study. PLoS Comput Biol. 2015 Apr 17;11(4):e1004180.
[3]. Tam VH, et al. In vitro potency of various polymyxin B components. Antimicrob Agents Chemother. 2011 Sep;55(9):4490-1.
[4]. Alonso MA, et al. Compounds affecting membranes that inhibit protein synthesis in yeast. Antimicrob Agents Chemother. 1979 Dec;16(6):750-6.
[5]. Sivanesan S, et al. Pharmacokinetics of the Individual Major Components of Polymyxin B and Colistin in Rats. J Nat Prod. 2017 Jan 27;80(1):225-229.