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首页-小分子抑制剂&激动剂-Antibiotics and Antivirals-Bacterial

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Bacteria constitute a large domain of prokaryoticmicroorganisms. Antibiotics (also called antibacterials) are a type of antimicrobial drug used in the treatment and prevention of bacterial infections, a limited number of antibiotics also possess antiprotozoal activity. Together with vaccination, antibiotics have led to the near eradication of diseases such as tuberculosis in the developed world. However, their effectiveness and easy access have also led to their overuse, prompting bacteria to develop resistance.

A bactericidal activity of antibacterials may depend on the bacterial growth phase, and it often requires ongoing metabolic activity and division of bacterial cells. In vitro characterization of antibacterial activity commonly includes the determination of the minimum inhibitory concentration and minimum bactericidal concentration of an antibacterial. To predict clinical outcome, the antimicrobial activity of an antibacterial is usually combined with its pharmacokinetic profile, and several pharmacological parameters are used as markers of drug efficacy.

 
 

Cat. No. Product Name Information
PC-22567

OXF-077

Antibacterial agent

OXF-077 is a potent inhibitor of the mutagenic SOS response, suppresses the rate of ciprofloxacin resistance emergence in S. aureus, is a potentiator of DNA-damage in MRSA.
PC-22557

Ciprofloxacin

Antibiotic

Ciprofloxacin (Bay-09867) is a potent, orally active topoisomerase IV inhibitor and fluoroquinolone antibiotic, induces mitochondrial DNA and nuclear DNA damage and lead to mitochondrial dysfunction, ROS production.
PC-22556

LEI-800

Bacterial DNA gyrase inhibitor

LEI-800 is potent antibacterial as an allosteric bacterial topoisomerase DNA gyrase inhibitor with MIC of 3.1 uM and 6.25 uM for E. coli and K. pneumoniae respectively, inhibits the ATP-dependent supercoiling activity of recombinant E. coli DNA gyrase in a gel-based assay with IC50 of 35 nM.
PC-22548

D8-03

Francisella tularensis inhibitor

D8-03 is a potent inhibitor of intracellular growth of Francisella tularensis with IC50 of 15 nM in CFU assays, MIC50 value of 0.39 uM.
PC-22508

ECIN (E. coli inhibitor)

UPEC inhibitor

ECIN (E. coli inhibitor) is a copper-responsive small molecule inhibitor of wild-type uropathogenic Escherichia coli (UPEC) strains with IC50 of 336 ng/mL in the absence of copper, and 260 and 128 ng/mL in the presence of 25 and 250 µM copper, respectively.
PC-22507

A16B1

Salmonella PhoP/PhoQ inhibitor

A16B1 is a specfic, allosteric inhibitor of the PhoQ histidine kinase, selectively inhibits the activity of the Salmonella PhoP/PhoQ system, blocks Salmonella pathogenicity.
PC-22472

BTZ043

DprE1 inhibitor

BTZ043 is a small molecule antimycobacterial agent taregting the DprE1 (Rv3790) subunit of the enzyme decaprenylphosphoryl-beta-d-ribose 2'-epimerase, shows MIC values of 1 ng/ml (2.3 nM) and 4 ng/ml (9.2 nM) against M. tuberculosis H37Rv and Mycobacterium smegmatis, respectively.
PC-22350

Cadazolid

Antibiotic

Cadazolid (ACT-179811) is a first-in-class quinoxolidinone antibiotic and a potent inhibitor of C. difficile protein synthesis with IC50 of 0.38 uM in in vitro transcription/translation assay, MIC of <0.03 ug/mL against Clostridioides difficile ATCC 700057.
PC-22242

Pneumolysin inhibitor PB-3

Pneumolysin inhibitor

Pneumolysin inhibitor PB-3 is a specific small molecule inhibitor (pore-blocker) of pneumolysin (PLY), binds to Cys428 adjacent to the cholesterol recognition domain of PLY with KD of 256 nM, block the PLY-induced hemoglobin release in sheep erythrocytes with IC50 of 3.1 uM.
PC-22210

Cerastecin D

MsbA inhibitor

Cerastecin D is a potent small molecule inhibitor of A. baumannii transporter MsbA, is a potent and bactericidal against A. baumannii, including clinical carbapenem-resistant Acinetobacter baumannii isolates.
PC-22209

Cerastecin C

MsbA inhibitor

Cerastecin C is a potent small molecule inhibitor of A. baumannii transporter MsbA, is a potent and bactericidal against A. baumannii, including clinical carbapenem-resistant Acinetobacter baumannii isolates.
PC-22208

Cerastecin B

MsbA inhibitor

Cerastecin B is a potent small molecule inhibitor of A. baumannii transporter MsbA with binding KD of 0.37 nM, is a potent and bactericidal against A. baumannii, including clinical carbapenem-resistant Acinetobacter baumannii isolates.

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