Antimicrobianos

Kanamycin is a broad spectrum antibiotic active against both gram-positive and gram-negative bacteria. It is used to treat severe infections including sepsis and tuberculosis. It  is another selection agent commonly used to screen bacteria, such as, E. coli, but also suitable for yeast specie,s such as, P. pastoris and plastid transformation of tobacco.

Vidarabine monohydrate is an antiviral agent with action on viral DNA polymerase to inhibit replication and is used for treating herpes simplex virus infections and varicella-zoster virus infections.

Clindamycin 3-phosphate is an antibiotic prodrug, which is a derivative of clindamycin. It is semisynthetic with a synthetic origin, derived by chemically modifying the natural compound lincomycin obtained from the bacterium *Streptomyces lincolnensis*. The mode of action of Clindamycin 3-phosphate involves the inhibition of bacterial protein synthesis. It binds to the 50S subunit of the bacterial ribosome, thereby interfering with the translocation step in protein elongation, ultimately leading to the suppression of bacterial growth. The primary uses and applications of Clindamycin 3-phosphate are in the treatment of infections caused by susceptible strains of anaerobic bacteria and certain gram-positive cocci. It is utilized in both topical and systemic formulations, with systemic applications including the treatment of serious infections such as those occurring in the lower respiratory tract, skin, and soft tissues. Clindamycin 3-phosphate's role as a prodrug is significant, as it undergoes hydrolysis in vivo to yield active clindamycin, ensuring effective delivery and action within the host system.

Ciprofloxacinhydrochloride, the hydrochloride salt form of ciprofloxacin is afluoroquinolone that exerts its antibacterial activity by inhibiting DNK gyrase (topoisomerase II) which inhibits relaxation of supercoiled DNA and promotes breakage of double-stranded DNA. Also, ciprofloxacine inhibits cytochrome P450 CYP1A2. Ciprofloxacine is a broad spectrum antibiotic,effective against Gram positive and Gram negative bacteria: Enterobacteriaceae, H. influenzae, N. gonorrhoeae, Campylobacter spp and Pseudomonas with clinical application for complicated urinary tract infections, respiratory infections caused by Pseudomonas aeruginosa strains inpatients with cystic fibrosis, invasive otitis externa caused by P. aeruginosa, chronic osteomyelitis caused by gram negative organisms, eradication of Salmonella, gonorrhoea, bacterial prostatitis, cervicitis, anthrax.

Tri-O-benzyl FR 900098 is a chemical compound, often referenced in biochemical research contexts. It is a synthetic derivative that originates from complex chemical synthesis, involving multiple benzylation steps to modify the original molecular framework. This structural transformation lends the compound unique chemical properties. The mode of action of Tri-O-benzyl FR 900098 involves interactions at a molecular level, often serving as a substrate or an inhibitor in enzymatic studies. Its distinctive benzylated structure allows it to fit into active sites of enzymes with high specificity, enabling researchers to study enzyme activity, inhibition, and protein-ligand interactions. In terms of applications, Tri-O-benzyl FR 900098 is utilized extensively in the field of enzymology and structural biology. Its properties make it an ideal candidate for probing enzyme mechanisms, testing hypotheses related to enzyme specificity, and studying the impacts of structural modifications on activity. This compound thus plays a crucial role in advancing our understanding of biochemical pathways and the development of novel therapeutics.

Inhibitor of RNA polymerases; inhibitor of HSP27-cytoskeleton interactions

Posaconazole is an antifungal agent that inhibits the 14-alpha demethylase enzyme which is responsible for the synthesis of the fungal cell wall component, ergosterol. This demethylase enzyme synthesizes ergosterol through converting lanosterol to ergosterol. Therefore Posaconazole prevents the formation of fungal cell walls with the appropriate membrane permeability thus leading to fungal cell lysis. Posaconazole can be used as an antifungal drug to treat opportunistic fungal infections in immunocompromised individuals such as HIV patients. Moreover it is shown to inflict its inhibitory activity against common pathogenic fungus such as Candida and Aspergillus species but also Mucorales and some Fusarium species, which are less common.

Bottromycin A2 is a peptide antibiotic, which is a natural product derived from the fermentation of certain Streptomyces strains. It operates by targeting the bacterial ribosome, specifically inhibiting protein synthesis. The mode of action involves binding to the A-site of the 50S ribosomal subunit, thereby preventing the correct positioning of transfer RNA (tRNA) during translation. This inhibition halts the growth of bacteria by disrupting essential protein production processes. Bottromycin A2 is primarily applied in research settings focused on combating antibiotic-resistant bacteria. Its unique structure and mode of action make it a candidate for studying novel mechanisms to overcome bacterial resistance, particularly against Gram-positive organisms. Further investigations into Bottromycin A2 can inform the development of new therapeutic agents and provide insights into ribosomal function and inhibition.

Abacavir-d4 is a deuterium-labeled analogue of the antiretroviral medication Abacavir. It serves as a critical tool for pharmaceutical research and development. This isotopically labeled compound is synthesized by incorporating four deuterium atoms into the molecular structure of Abacavir, preserving the pharmacokinetic and pharmacodynamic properties of the original molecule while allowing for precise analytical quantification. In practice, Abacavir-d4 functions as an internal standard in mass spectrometric analyses. Its mode of action, akin to its unlabeled counterpart, involves the inhibition of reverse transcriptase, thereby hindering the replication of HIV-1. The deuterium labeling, however, does not alter its biological activity but provides a stable reference point for accurately measuring Abacavir concentrations in biological samples using high-performance liquid chromatography coupled with tandem mass spectrometry (HPLC-MS/MS). Primarily utilized in laboratory settings, Abacavir-d4 aids in the pharmacokinetic and metabolic studies of Abacavir, enhancing the reliability and accuracy of the data obtained. Its precise quantitation capabilities are indispensable in advancing understanding of drug metabolism and optimizing therapeutic strategies against HIV.

Tebufenozide-hydroxymethyl is an insect growth regulator, which is synthesized chemically to function as an agonist of the molting hormone, ecdysone, in target pest species. It operates by mimicking the effects of ecdysone, leading to premature and lethal molting in lepidopteran larvae. This disruption in the developmental cycle of the insects effectively suppresses their population by preventing them from reaching maturity and reproducing. In agricultural applications, Tebufenozide-hydroxymethyl is utilized to manage pest infestations in a variety of crops, including fruits, vegetables, and ornamentals. Its specific action against immature stages of lepidopterans makes it a valuable tool in integrated pest management systems, where it is used to minimize the reliance on broad-spectrum insecticides. By selectively targeting pests without significantly impacting beneficial insects and pollinators, it contributes to sustainable agricultural practices.

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Tiamulin fumarate is a pleuromutilin antibiotic with action on bacterial protein synthesis by targeting the 50S ribosomal subunit and is used for treating swine dysentery and respiratory infections in livestock.

Actinomycin D is an antibiotic commonly used in chemotherapy for cancer treatment, such as sarcomas, and pediatric solid tumors, Wilm’s tumor, testicular cancer, and choriocarcinoma; it is generally not very useful in antibiotic therapy. It acts as a transcription inhibitor, binding to DNA duplexes at the transcription initiation complex and preventing RNA polymerase elongation.

Applications Thymol O-β-D-Glucuronide is a glucuronide derivative of Thymol (T413000); an antimicrobial compound which can increase the efficacy of antibiotics involving drug resistant bacteria. It inhibits growth and lactate production as well as reduces cellular glucose uptake within the bacteria. References Palaniappan, K. et al.: Int. J. Food Microbiol., 140, 164 (2010); Evans, J. et al.: Curr. Microbiol., 41, 336 (2000)

PF 1022A is a cyclooctadepsipeptide, which is a type of cyclic peptide composed of amino acids and hydroxy acids. It is derived from the fermentation products of the fungus *Mycelia sterilia*, a member of the *Rosellinia* genus. Its mode of action involves disrupting glutamate-gated chloride channels in parasitic nematodes, which leads to paralysis and eventual death of the parasite. PF 1022A is primarily used for its anthelmintic properties, making it useful for controlling parasitic worm infections in animals. The compound's ability to selectively target nematodes without significant harm to the host organism makes it a valuable tool in veterinary medicine. It serves as a key component in formulations designed to combat gastrointestinal nematodes in livestock and pets, contributing to enhanced health and productivity in affected animals. Research into PF 1022A continues to explore its full potential and further applications in parasitology.

Inhibitor of DNA replication; aminoglycoside class

Vancomycin is a tricyclic glycopeptide antibiotic that has bactericidal effects against staphylococci, streptococci, and other gram-positive bacteria. It is often used as an alternative treatment for severe staphylococcal and streptococcal infections, including endocarditis, and infections with MRSA (methicillin-resistant Staphylococcus aureus), penicillin-resistant pneumococci or in cases of allergy to penicillins and cephalosporins.

Broad-spectrum antibiotic; bacterial cell wall biogenesis inhibitor

Benznidazole is an antiprotozoal agent and is used for the treatment of Chagas disease. It generates free radicals that damage the DNA and other cellular components of the parasite.

Tris(4'-carboxy-1,1'-biphenyl)amine is an organic compound commonly employed as a building block in the development of advanced materials. It is synthesized through a series of chemical reactions involving biphenyl and aniline derivatives, ultimately producing a triphenylamine core with carboxylic acid functional groups. The unique molecular architecture allows this compound to participate in various chemical interactions, including π-π stacking and hydrogen bonding, which are pivotal in its applications. The mode of action of Tris(4'-carboxy-1,1'-biphenyl)amine is primarily based on its ability to facilitate charge transport and enhance electronic coupling. This makes it an essential component in the formulation of organic semiconductors, where its structural attributes contribute to improved performance in electronic devices. Notably, Tris(4'-carboxy-1,1'-biphenyl)amine is utilized in the fabrication of organic light-emitting diodes (OLEDs), photovoltaic cells, and field-effect transistors. Its role is crucial in enhancing the efficiency and stability of these devices, making it a valuable material in cutting-edge optoelectronic research and development.

Cefoselis hydrochloride is a broad-spectrum antibiotic, which is a synthetic cephalosporin derived from a semi-synthetic process involving modifications of naturally occurring cephalosporin C. Its mode of action involves inhibiting bacterial cell wall synthesis by binding to specific penicillin-binding proteins, leading to cell lysis and death. Cefoselis hydrochloride is specifically effective against a wide range of Gram-positive and Gram-negative bacteria, including strains resistant to other cephalosporins. Its potent activity comes from its strong affinity for the target proteins and its resistance to certain beta-lactamases. This antibiotic is applied in clinical settings to treat severe infections, such as pneumonia, sepsis, and complicated urinary tract infections, especially where multidrug-resistant bacteria are involved. Due to its efficacy and safety profile, cefoselis hydrochloride is a crucial drug in the arsenal against bacterial infections in both hospital and outpatient environments.

Applications Ethyl Paraben-d4 is the labeled analogue of Ethyl Paraben (E925475), an antimicrobial agent used in cosmetic products. References Gilliland, D., et al.: J. Appl. Bacteriol., 72, 258 (1992), Routledge, E., et al.: Toxicol. Appl. Pharmacol., 153, 12 (1998), Miller, C., et al.: J. Biol. Chem., 272, 32824 (1997), Nakagawa, Y., et al.: Biochem. Pharmacol., 55, 1907 (1998),

Broad spectrum imidazole antifungal

Licoflavone B is a naturally occurring flavonoid, which is primarily derived from the roots of licorice plants, such as Glycyrrhiza inflata. It functions as a bioactive compound with potential antioxidant and anti-inflammatory activities. The mode of action of Licoflavone B involves the scavenging of free radicals, modulation of signaling pathways, and inhibition of pro-inflammatory mediators. These biological activities render it valuable in research focused on chronic diseases and oxidative stress. The applications of Licoflavone B are expansive within the scientific and medical research communities. It is especially pertinent in studies aiming to elucidate the molecular mechanisms underlying its beneficial effects on cell biology. This flavonoid's potential therapeutic benefits are under investigation for conditions such as cardiovascular diseases, cancer, and neurodegenerative disorders. By exploring its interactions at the cellular level, researchers strive to harness its properties for developing novel treatments and preventive strategies against oxidative damage and inflammation-related pathologies.

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JNJ-4796 is an antiviral compound with a mode of action that inhibits hemagglutinin-mediated fusion in influenza A viruses. It is used for preventing and treating influenza infections.

Cefepime-d3 sulfate is an isotopically labeled antibiotic, which is derived from the fourth-generation cephalosporin, cefepime. The source of this compound is synthetic, utilizing deuterium to label the parent cefepime molecule, allowing for detailed metabolic and pharmacokinetic studies. With deuterium's stable, non-radioactive nature, it serves as a powerful tool in mass spectrometry-based analyses. The mode of action of cefepime-d3 sulfate involves inhibiting bacterial cell wall synthesis, similar to the mechanism observed in other β-lactam antibiotics. It achieves this by binding to penicillin-binding proteins, disrupting the final stages of peptidoglycan cross-linking in bacterial cell walls, ultimately leading to cell lysis and death. Cefepime-d3 sulfate finds its applications predominantly in research settings. Scientists utilize it to investigate bacterial resistance mechanisms, determine metabolic pathways, and analyze drug distribution and clearance rates within biological systems. Its isotopic labeling enhances the precision of such studies, providing insights that guide the development of new antibacterial strategies and resistance mitigation approaches. These investigations are crucial in an era where antibiotic resistance poses a significant global health threat.

Nortadalafil-N-(2-hydroxy)propyl is a chemotherapeutic agent, which is synthesized through the chemical modification of tadalafil. It is characterized as a small-molecule inhibitor, derived from the structural alteration of the well-known phosphodiesterase type 5 (PDE5) inhibitor. The mechanism of action involves the attenuation of PDE5 activity, leading to increased levels of cyclic guanosine monophosphate (cGMP) within targeted cellular pathways. This elevation in cGMP concentration results in vasodilation and increased blood flow, primarily investigated within the context of vascular and erectile tissue. The compound's applications extend potentially beyond its predecessor, tadalafil, with research focusing on improved pharmacokinetics and selectivity. Scientists are exploring its utility in treating conditions such as pulmonary arterial hypertension and other vascular disorders. Current investigations are assessing its efficacy, bioavailability, and potential side-effect profile, with the aim of expanding its therapeutic margin and optimizing clinical outcomes. This innovative drug design signifies an advancement in molecular pharmacology, offering opportunities for enhanced treatment paradigms in cardiovascular medicine.

Nifursemizone is an antimicrobial agent, which is a synthetic nitrofuran derivative. It is engineered from chemical precursors through targeted synthetic processes designed to maximize its antibacterial properties. The mode of action of Nifursemizone involves the inhibition of bacterial enzymes and interference with nucleic acid synthesis. This action disrupts essential bacterial functions, leading to the inhibition of bacterial growth and eventual cell death. Nifursemizone is primarily utilized in veterinary medicine as an antibacterial treatment for livestock. Its application is particularly valuable in managing gastrointestinal infections and systemic bacterial diseases in animals. The compound's efficacy against a broad spectrum of Gram-positive and Gram-negative bacteria positions it as a critical tool for ensuring the health and productivity of animal populations. Nifursemizone's role in antimicrobial strategies is noteworthy for its targeted approach and effectiveness in clinical veterinary contexts, providing a significant contribution to bacterial infection management.

Applications A 6-substituted 8-quinolinecarboxylic acid as antimicrobial and genotoxic agent. References Weyer, R., et al.: Arzneim.-Forsch., 24, 269 (1974),

MMV008138 is an antimalarial compound, which is a synthetic chemical entity derived from medicinal chemistry efforts aimed at targeting malaria. The source of MMV008138 is the pharmaceutical research pipeline focused on identifying new antimalarial agents. It operates by inhibiting the Plasmodium falciparum enzyme PfNDH2, an essential component in the parasite’s respiratory chain, disrupting its energy production capabilities and ultimately leading to parasite death. The primary use of MMV008138 is in the experimental treatment of malaria, a disease caused by Plasmodium parasites, with an emphasis on strains resistant to current treatments. In preclinical models, MMV008138 has shown promising activity against both erythrocytic and hepatic stages of the parasite’s life cycle. These characteristics suggest its potential as part of combination therapies, addressing the global challenge of drug-resistant malaria. It is under ongoing study to determine its pharmacokinetics, safety profile, and efficacy in humans, with the ultimate goal of contributing to novel therapeutic regimens aimed at malaria eradication.

Moxifloxacin is a synthetic broad-spectrum antibiotic, which is derived from the fluoroquinolones class. It functions by inhibiting bacterial topoisomerase II (DNA gyrase) and topoisomerase IV, enzymes critical for DNA replication, transcription, repair, and recombination. The inhibition of these enzymes results in DNA breakage, thereby leading to bacterial cell death. Moxifloxacin exhibits potent activity against a wide variety of Gram-positive and Gram-negative organisms. It is particularly effective against respiratory pathogens, including multidrug-resistant Streptococcus pneumoniae. Additionally, this compound is utilized in the treatment of bacterial skin infections, complicated intra-abdominal infections, and acute bacterial sinusitis, among others. Due to its robust ability to penetrate tissues and its broad-spectrum efficacy, moxifloxacin is a valuable pharmacological option in the management of severe bacterial infections, where resistant organisms are of clinical concern.

Marbofloxacin is an antibiotic belonging to the class of fluoroquinolones. It is used in veterinary medicine to treat bacterial infections in animals. This drug inhibits the bacterial enzyme DNA gyrase and topoisomerase IV. As a result, this drug prevents bacterial DNA replication. Marbofloxacin is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready-to-use products for assay development, screening or other R&D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.

Ofloxacin methyl ester is a chemical compound, which is a derivative utilized in scientific research, particularly in the synthesis of ofloxacin-related compounds. It is a synthetic ester, derived from chemical synthesis involving ofloxacin, a fluoroquinolone antibiotic. The mode of action of ofloxacin methyl ester is based on its role as an intermediate compound. It facilitates the creation of active forms or analogs that can be tested for their pharmacological properties. Although not directly used as a therapeutic agent, it plays a crucial role in the development and modification of molecules for antibacterial applications. This compound is primarily applied in research settings to explore the effectiveness and enhancement of fluoroquinolone antibiotics. Its use extends to investigating the structure-activity relationships and optimizing new compounds that may possess improved antibacterial activity or reduced resistance profiles. The importance of ofloxacin methyl ester lies in its ability to drive innovation in antibiotic therapy, contributing to our understanding of drug development and microbial resistance mechanisms.

Gatifloxacin hydrate is a fluoroquinolone antibiotic, which is synthesized chemically. It exerts its bactericidal effects primarily by inhibiting bacterial DNA gyrase and topoisomerase IV. These enzymes are crucial for bacterial DNA replication, transcription, and repair. By preventing these processes, gatifloxacin effectively halts bacterial cell division, ultimately leading to cell death. Gatifloxacin hydrate is utilized extensively in the treatment of various bacterial infections, particularly those affecting the respiratory tract, skin, and urinary tract. Its broad-spectrum activity ensures it is effective against both Gram-positive and Gram-negative bacteria. Given its potent antibacterial properties, gatifloxacin is a valuable tool in managing infections that are resistant to other antibiotics, particularly in clinical settings. Proper utilization and adherence to prescribed regimens are essential to maintaining its efficacy and mitigating resistance development.