Rifampicin-d3 (Synonyms: Rifampin-d3)

Rifampicin-d₃ is intended for use as an internal standard for the quantification of rifampicin by GC- or LC-MS. Rifampicin is a rifamycin antibiotic and inhibitor of bacterial RNA polymerase (IC₅₀ = 0.01 μg/ml for the E. coli enzyme).¹ It inhibits the growth of M. tuberculosis H37Rv in mouse peritoneal macrophages (MIC = 0.8 μg/ml) as well as clinical isolates of various species of Staphylococcus, Streptococcus, Haemophilus, and Neisseria (MICs = 0.009-1.4 μg/ml).^2,3 Rifampicin increases survival in a mouse model of tuberculosis infection.³ It is also an agonist of the human pregnane X receptor (PXR; EC₅₀ = ~2 μM).⁴ Formulations containing rifampicin have been used in the treatment of tuberculosis and meningococcal carriers.

1.Wehrli, W.Rifampin: Mechanisms of action and resistanceRev.Infect.Dis.5(3)S407-S411(1983) 2.Jhamb, S.S., Goyal, A., and Singh, P.P.Determination of the activity of standard anti-tuberculosis drugs against intramacrophage Mycobacterium tuberculosis, in vitro: MGIT 960 as a viable alternative for BACTEC 460Braz. J. Infect. Dis.18(3)336-340(2014) 3.Arioli, V., Berti, M., Carniti, G., et al.Antibacterial activity of DL 473, a new semisynthetic rifamycin derivativeJ. Antibiot. (Tokyo)34(8)1026-1032(1981) 4.Gill, S.K., Xu, H., Kirchhoff, P.D., et al.Structure-based design of novel benzoxazinorifamycins with potent binding affinity to wild-type and rifampin-resistant mutant Mycobacterium tuberculosis RNA polymerasesJournal of Medicinal Chemistry55(8)3814-3826(2012)