Maraviroc is a selective CCR5 antagonist with activity against human HIV.
Human milk lysozyme is the lysozyme found in human milk. Human milk lysozyme is thought to be a key defense factor in protecting the gastrointestinal tract of newborns against bacterial infection[1].
PLpro inhibitor is a potent inhibitor of papain-like protease (PLpro) with IC50 of 2.6 uM.IC50 Value: 2.6 uM [1]Target: PLpro; SARS-CoVin vitro: PLpro inhibitor is a potent inhibitor against the papain-like protease (PLpro) from the coronavirus that causes severe acute respiratory syndrome (SARS-CoV). PLpro inhibitor was found to have IC50 value of 2.6 ± 0.1 μM. PLpro inhibitor display significant antiviral activity with EC50 values of 13.1±0.7 uM, without toxicity up to the highest concentration tested. Notably, the increasing antiviral potency correlates with the in vitro inhibition of PLpro, suggesting that the compounds work directly on the enzyme in cells [1,2].in vivo:
Sulfamerazine D4 is a deuterium labeled Sulfamerazine. Sulfamerazine, a sulfonamide antibacterial, inhibits bacterial synthesis of dihydrofolic acid by competing with para-aminobenzoic acid (PABA) for binding to dihydropteroate synthesizes[1].
Coreoside B (14-Hydroxycoreoside A) can be isolated from Coreopsis tinctoria Nutt. and has weak antibacterial activity[1].
Avermectin B1 (Abamectin) is a widely used insecticide and anthelmintic. IC50 Value: N/ATarget: AntiparasiticAvermectin B1 is a mixture of avermectins containing more than 80% avermectin B1a and less than 20% avermectin B1b. These two components, B1a and B1b have very similar biological and toxicological properties. The avermectins are insecticidal and antihelmintic compounds derived from various laboratory broths fermented by the soil bacterium Streptomyces avermitilis. Avermectin B1 is a natural fermentation product of this bacterium.
Albomycin is an inhibitor of aminoacyl-tRNA synthetases with Trojan-horse effect. Albomycin is delivered by iron-chelator portion into bacterial through ferrichrome-specific transporter system. Albomycin combats against a wide range of Gram-positive and Gram-negative bacteria. Albomycin also serves as an efficient iron-scavenger of producer[1].
Chitin synthase inhibitor 2 (compound 2b) is a potent inhibitor of chitin synthase with the IC50 value of 0.09 mM and the Ki value of 0.12 mM. Chitin synthase inhibitor 2 has antimicrobial activities in vitro and shows synergistic or additive effects with fluconazole or polyoxin B[1].
Levofloxacin-13C,d3 is the 13C- and deuterium labeled.
FPI-1523 sodium, a derivative of Avibactam, is a potent β-lactamase inhibitor, with Kds of 4 nM and 34 nM for CTX-M-15 and OXA-48, respectively. FPI-1523 sodium also inhibits PBP2, with an IC50 of 3.2 μM. FPI-1523 sodium exhibits considerable antimicrobial activity[1].
Pefloxacin is a an antibacterial agent and prevents bacterial DNA replication by inhibiting DNA gyrase (topoisomerse)Target: DNA gyrasePefloxacin is a synthetic chemotherapeutic agent used to treat severe and life-threatening bacterial infections. Pefloxacin is commonly referred to as afluoroquinolone (or quinolone) drug and is a member of the fluoroquinolone class of antibacterials. It is an analog of norfloxacin. It is a synthetic fluoroquinolone, belonging to the 3rd generation of quinolones. Pefloxacin is extensively prescribed in France. Pefloxacin has not been approved for use in the United States.The bactericidal action of pefloxacin results from interference with the activity of the bacterial enzymes DNA gyrase and topoisomerase IV, which are needed for the transcription and replication of bacterial DNA. DNA gyrase appears to be the primary quinolone target for gram-negative bacteria. Topoisomerase IV appears to be the preferential target in gram-positive organisms. Interference with these two topoisomerases results in strand breakage of the bacterial chromosome, supercoiling, and resealing. As a result DNA replication and transcription is inhibited.
Antibiotic-5d is a synthesis and antimicrobial compound.
Pyridoxal phosphate-d5 (Pyridoxal 5′-phosphate-d5) is the deuterium labeled Pyridoxal phosphate. Pyridoxal phosphate is the active form of vitamin B6, acts as an inhibitor of reverse transcriptases, and is used for the treatment of tardive dyskinesia[1][2].
Nifeviroc is an orally active CCR5 antagonist. Nifeviroc is used for the study of HIV type-1 infection[1].
N-Butanoyl-L-homoserine lactone is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). N-Butanoyl-L-homoserine lactone has antibacterial activity and is used in antibacterial biofilm[1].
Anti-Influenza agent 4 is a potent and selective influenza virus inhibitor with EC50s of 150 nM and 62 nM for strains A/Roma and A/Parma, respectively[1].
Chlorhexidine acetate hydrate is an antibacterial used as an antiseptic and for other applications. Chlorhexidine acetate hydrate is used to clean the skin after an injury, before surgery, or before an injection. Chlorhexidine acetate hydrate is also used to clean the hands before a procedure[1].
G0507, a pyrrolopyrimidinedione compound, is a potent LolCDE ABC Transporter inhibitor. G0507 is a inhibitor of Escherichia coli growth and induces the extracytoplasmic σE stress response. G0507 acts as a chemical probe to dissect lipoprotein trafficking in Gram-negative bacteria[1].
Plonmarlimab (TJ003234) is an anti-GM-CSF monoclonal antibody. Plonmarlimab can be used for research of rheumatoid arthritis and COVID-19[1][2].
Acyclovir (Aciclovir) sodium is a potent, orally active antiviral agent. Acyclovir sodium has antiherpetic activity with IC50 values of 0.85 μM and 0.86 μM for HSV-1 and HSV-2, respectively. Acyclovir sodium induces cell cycle perturbation and apoptosis. Acyclovir sodium prevents bacterial infections during induction therapy for acute leukaemia[1][2][3][4].
5-desmethylsinensetin, isolated from Stevia satureiifolia var. satureiifolia, possesses antiprotozoal activity. 5-desmethylsinensetin shows IC50 values of 0.4 μg/mL on T. cruzi epimastigotes and 75.1 μg/mL on trypomastigotes, respectively[1].
Kanamycin sulfate is an aminoglycoside bacteriocidal antibiotic which acts by binding to the bacterial 30S ribosomes.
AL-9 is a small molecule HCV replication inhibitor with EC50 of 0.29 and 0.75 uM for genotype 1b and 2a, inhibits purified PI4KIIIα with IC50 of 0.57 uM; inhibits HCV across different genotypes with activity in the sub-micromolar to low micromolar range in the absence of significant cytotoxic effects; inhibits PI4KIIIα also in living cells, while not appreciably affecting the activity of PI4KIIIβ, does not affect the level of PI4P in the Golgi membrane.
HBV-IN-41 (compound 45) is a potent and orally active Hepatitis B Virus (HBV) inhibitor, with an EC50 of 0.027μM[1].
Lacto-N-tetraose is the significant core structure of human milk oligosaccharides (HMOs) naturally existing in human milk. Lacto-N-tetraose is consist of galactose, N-acetylglucosamine, and glucose moieties. Lacto-N-tetraose has prebiotic effect, immune regulatory effect, anti-inflammatory effects, intestinal cell responses regulatory effect, antibacterial activity and antiviral activity. Lacto-N-tetraose has been widely added to infant formula[1].
Antibacterial agent 12, a biaryloxazolidinone analogue, is an antibacterial agent against antibiotic-susceptible and antibiotic-resistant Gram-positive bacteria[1].
Cratoxylone, isolated from the bark of Cratoxylum Cochinchinense, possesses antiplasmodial activity[1][2].
HIV p17 Gag (77-85) is an HLA-A*0201(A2)-restricted CTL epitope, used in the research of anti-HIV[1].
Antifungal agent 34 (compound 6i) is a potent antifungal agent. Antifungal agent 34 shows a potent antifungal activity against Candida albicans, with a MIC of 4 µg/mL. Antifungal agent 34 shows significant inhibition on Candida albicans hyphae and biofilm development. Antifungal agent 34 exhibits no cytotoxicity to mammalian cells[1].
Fluorescein Di-β-D-Glucuronide, a fluorescent probe, can be utilized to non-invasively image the intestinal bacterial β-glucuronidase activity in nude mice. Fluorescein Di-β-D-Glucuronide-based imaging reveals the in vitro and in vivo activity of intestinal bacterial β-glucuronidase, which would facilitate pharmacodynamic studies of specific bacterial β-glucuronidase inhibitors in animal studies[1].