The pristinamycins exhibit a strong synergistic antibacterial activity against a wide range of Gram-positive and some Gram-negative bacteria, including methicillin- and vancomycin-resistant strains. Pristinamycin is an effective, well-tolerated alternative therapeutic option in MSSA BJI, on condition that a daily dosage of 50 mg/kg is respected.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||10 mM in DMSO|
Pristinamycin in the treatment of MSSA bone and joint infection.
Valour F, et al. J Antimicrob Chemother. 2016 Apr;71(4):1063-70. PMID: 26801082.
A Complex Signaling Cascade Governs Pristinamycin Biosynthesis in Streptomyces pristinaespiralis.
Mast Y, et al. Appl Environ Microbiol. 2015 Oct;81(19):6621-36. PMID: 26187956.
Glutaminase C-IN-1 (968) is an allosteric inhibitor of Glutaminase C that inhibits cancer cell growth without affecting their normal cellular counterparts.
NSC 23766 is an inhibitor of Rac GTPase targeting Rac activation by guanine nucleotide exchange factors (GEFs) with IC50 of ~50 μM in a cell-free assay; does not inhibit the closely related targets, Cdc42 or RhoA.
Budesonide is a GC steroid commonly used for the treatment of asthma and non-infectious rhinitis.
Brequinar is a potent inhibitor of dihydroorotate dehydrogenase, with potent activities against a broad spectrum of viruses.
Laropiprant is a potent, selective DP1 receptor antagonist with Ki value of 0.57 nM, and exhibits > 1,000 fold selectivity over DP2 receptor (Ki=0.75 μM).
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