Cefazolin exhibits a broad spectrum of bioactivities, including significant antimicrobial activity against a variety of bacterial strains. Its antibacterial efficacy varies widely depending on the strain and resistance profile, with notable activity against methicillin-resistant Staphylococcus aureus (MRSA), Escherichia coli, Klebsiella pneumoniae, among others. The minimum inhibitory concentrations (MIC) for Cefazolin span from sub-microgram to high micromolar levels, indicating diverse potency across different bacterial targets.
Additionally, Cefazolin demonstrates dynamic hydrolysis rates under different pH conditions, with a higher rate of hydrolysis at more alkaline pH values, specifically pH 10 compared to pH 9.6. The compound also shows low binding affinity to the membrane transport protein PEPT1 in human Caco-2 cells and exhibits antiproliferative effects in various human cell lines, including primary human osteoblasts, MG63 cells, and HeLa cells.
In terms of pharmacokinetic properties, Cefazolin has a high oral bioavailability of 90% and favorable pharmacokinetics such as a volume of distribution at steady state of 0.1 L.kg-1, and a total body clearance of 0.89 mL.min-1.kg-1, indicating efficient absorption and moderate elimination from the body. The compound also shows significant protein binding in plasma and some degree of renal clearance.
Cefazolin has been observed to exhibit moderate liver toxicity during clinical trials, marked by elevated serum enzyme levels. It shows a broad range of activity in various bioassays, including those for transporter inhibition, bacterial efflux pump interactions, and activity against specific metabolic pathways and enzymes in pathogenic organisms. The compound also displays potential antiviral properties, including inhibition of SARS-CoV-2 induced cytotoxicity in VERO-6 cells, albeit at high concentrations.
Overall, Cefazolin is characterized by extensive antimicrobial efficacy, dynamic pH-dependent hydrolysis, significant pharmacokinetic attributes, and potential antiviral effects, rendering it a compound of interest for further research and development in antimicrobial and antiviral therapeutics..
Note: Summary generated by AI, AI may be wrong some times, we do not provide any medical advice and only sell our product to accredited institution, Please cross-check with other sources, data source: chembl 