Oxacillin sodium salt exhibits a broad range of bioactivities, including significant antibacterial and antiviral properties. It demonstrates potent activity as an inhibitor of beta-lactamase in Enterobacter aerogenes, with a high relative inhibition value of 5000.0 compared to oxacillin sulfoxide, and shows efficacy against methicillin-resistant Staphylococcus aureus (MRSA) with MIC values as low as 0.25 ug/mL. Additionally, MIC values against other bacterial strains vary widely, from highly potent (≤ 0.39 ug/mL against Staphylococcus aureus) to less effective (> 128.0 ug/mL against certain penicillin-resistant strains).
In pharmacokinetic studies, the compound reaches a concentration of 41.1 ug/mL in rat blood within 3 minutes and displays varied absorption rates in rabbit blood (15.3 ug/mL after 5 minutes and 9.1 ug/mL after 10 minutes). It also possesses a calculated lipophilicity with a Log k value of 1.868.
In terms of antiviral activity, Oxacillin sodium salt shows inhibition of SARS-CoV-2 induced cytotoxicity in several cell lines, including VERO-6 and Caco-2 cells, although the inhibition rates are relatively low (0.08% and 3.58% respectively, at 10 uM). Furthermore, it inhibits the SARS-CoV-2 3CL-Pro protease with an inhibition percentage of 33.68% at 20µM.
Oxacillin sodium salt also impacts various biochemical pathways and targets, such as enhancing SMN2 splice variant expression with a potency of 501.2 nM, and inhibiting Aldehyde Dehydrogenase 1 (ALDH1A1) and AmpC Beta-Lactamase with potencies of 44668.4 nM and 5623.4 nM respectively. It exhibits a potent inhibitory effect on sodium fluorescein uptake in OATP1B1-transfected and OATP1B3-transfected CHO cells, with inhibition rates of 76.67% and 90.07% at 10 uM.
Lastly, Oxacillin sodium salt shows low inhibitory effects on human BSEP, MRP2, MRP3, and MRP4, with IC50 values greater than 133,000.0 nM, and demonstrates minimal impact on cell viability in Vero E6 cells infected with SARS-CoV-2. It also exhibits differential inhibition of human HDAC6 activity, with various effects depending on the peptide substrates used in enzymatic assays..
Note: Summary generated by AI. Data source: ChEMBL 