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.
BMS-5 is a Potent LIM kinase inhibitor (IC50 values are 7 and 8 nM for LIMK1 and LIMK2 respectively).Inhibits cofilin phosphorylation in MDA-MB-231 breast cancer cells. Reduces MDA-MB-231 tumor cell invasion in a 3D matrigel invasion assay.
BMS-3 is a potent inhibitor of LIMK1.LIM kinase 1 (LIMK1) activity is essential for cell migration and cell cycle progression.
E7046 is an orally bioavailable and specific EP4 antagonist, with IC50 of 13.5 nM and Ki of 23.14 nM, exhibiting anti-tumor activities.
PF-05175157 (Compound 9) is a potent Acetyl-CoA carboxylase (ACC1) inhibitor with IC50s of 23.5±1.1 nM (rat) and 27.0±2.7 nM (human).
Epacadostat (INCB024360) is a potent and selective indoleamine 2,3-dioxygenase (IDO1) inhibitor with IC50 of 10 nM and displays high selectivity over other related enzymes such as IDO2 or tryptophan 2,3-dioxygenase (TDO).
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