Navafenterol (AZD-8871) saccharinate is an inhaled dual-acting, potent, selective, and long-lasting M3-antagonist/β2-agonist (MABA) with long-lasting effects and favorable safety profile. The pIC50 is 9.5 for human M3 receptor, and the pEC50 is 9.5 for β2-adrenoceptor. Navafenterol saccharinate can be used for the research of chronic obstructive pulmonary disease (COPD). Bronchoprotective and antisialagogue effects. Favorable cardiovascular profile[1].
HMMNI-d3 is deuterium labeled HMMNI. HMMNI (Hydroxy dimetridazole) is a hydroxy metabolite of Dimetridazole. Dimetridazole is a nitroimidazole class drug that combats protozoan infections[1].
Lymecycline is a tetracycline derivative, with broad-spectrum antibacterial activity and also has anti-inflammatory property.
Dalfopristin is a semi-synthetic streptogramin antibiotic. Quinupristin/Dalfopristin (Q/D) is a valuable alternative antibiotic to vancomycin for the treatment of multi-drug resistant Enterococcus faecium infections.
Aphidicolin is an inhibitor of DNA polymerase α and δ, prevents mitotic cell division by interfering with the activity of DNA polymerase[1].Aphidicolin is an antibiotic produced by the mold Cephalosporium aphidicola. Aphidicolin is a potent inhibitor of cellular deoxyribonucleic acid synthesis and inhibits the growth of herpes simplex virus[2].Aphidicolin potentiates apoptosis induced by arabinosyl nucleosides in a human promyelocytic leukemia cell line[3].
Miconazole Nitrate is an imidazole antifungal agent.Target: AntifungalMiconazole is an imidazole antifungal agent, developed by Janssen Pharmaceutica, commonly applied topically to the skin or to mucous membranes to cure fungal infections. It works by inhibiting the synthesis of ergosterol, a critical component of fungal cell membranes. It can also be used against certain species of Leishmania protozoa which are a type of unicellular parasite that also contain ergosterol in their cell membranes. In addition to its antifungal and antiparasitic actions, it also has some antibacterial properties. Miconazole is also used in Ektachrome film developing in the final rinse of the Kodak E-6 process and similar Fuji CR-56 process, replacing formaldehyde. Fuji Hunt also includes miconazole as a final rinse additive in their formulation of the C-41RA rapid access color negative developing process. From Wikipedia.
Itraconazole-d5 (R51211-d5) is the deuterium labeled Itraconazole. Itraconazole (R51211) is a triazole antifungal agent and a potent and orally active Hedgehog (Hh) signaling pathway antagonist with an IC50 of ~800 nM. Itraconazole potently inhibits lanosterol 14α-demethylase (cytochrome P450 enzyme), thereby inhibits the oxidative conversion of lanosterol to ergosterol. Itraconazole has anticancer and antiangiogenic effects[1][2][3].
Mezlocillin (BAY-f 1353) is a β-lactam antibiotic, a semisynthetic and extended-spectrum antibiotic. Mezlocillin is active against both gram-negative and gram-positive bacteria. Mezlocillin can be used in bacterial infection research[1][2].
Isobonducellin is a flavonoid product and shows antimicrobial activity[1].
ML406 is a small molecule probe that shows anti-tubercular activity via MtbbioA (DAPA synthase) enzyme inhibition with an IC50 of 30 nM[1].
Peldesine (BCX 34) is a potent, competitive, reversible and orally active purine nucleoside phosphorylase (PNP) inhibitor with IC50s of 36 nM, 5 nM, and 32 nM for human, rat, and mouse red blood cell (RBC) PNP, respectively. Peldesine is also a T-cell proliferation inhibitor with an IC50 of 800 nM. Peldesine has the potential for cutaneous T-cell lymphoma, psoriasis and HIV infection treatment[1][2][3][4].
Gliorosein is a fungal metabolite isolated from Gliocladium. Gliorosein is isomeric with the quinol but shows a different ultraviolet absorption spectrum[1].
Nifursemizone is an antiprotozoal drug.
(rac)-Modipafant-d4 (UK-74505-d4) is the deuterium labeled (Rac)-Modipafant. (Rac)-Modipafant (UK-74505) is an orally active, selective, long-acting irreversible platelet activating factor receptor (PAFR) antagonist. (Rac)-Modipafant prevents dengue infection[1][2][3].
SARS-CoV-2 3CLpro-IN-16 (Compound 3a) is a covalent SARS-CoV-2 3CLpro inhibitor (IC50s: 2.124 μM). SARS-CoV-2 3CLpro-IN-16 binds to the active site and forms a covalent bond with Cys145 of 3CLpro[1].
Saphenamycin is an antibiotic from a strain of Streptomyces.
Fosetyl-aluminum (Fosetyl-Al) is an active ingredient in many fungicides against downy mildew. Fosetyl-aluminum is used to control many diseases caused by Phytophthora spp. on agricultural and horticultural crops[1][2].
Gatifloxacin is an antibiotic of the fourth-generation fluoroquinolone family, it inhibits the bacterial enzymes DNA gyrase and topoisomerase IV.Target: AntibacterialGatifloxacin is an antibiotic of the fourth-generation fluoroquinolone family, that like other members of that family, inhibits the bacterial enzymes DNA gyrase and topoisomerase IV. Gatifloxacin had activity equal to that of tosufloxacin and activity more potent than those of norfloxacin, ofloxacin, ciprofloxacin, and sparfloxacin against the second-step mutants (grlA gyrA; gatifloxacin MIC range, 1.56 to 3.13 microg/ml) and had the most potent activity against the third-step mutants (grlA gyrA grlA; gatifloxacin MIC range, 1.56 to 6.25 microg/ml), suggesting that gatifloxacin possesses the most potent inhibitory activity against singly mutated topo IV and singly mutated DNA gyrase among the quinolones tested [1].Ophthalmic gatifloxacin 0.3% is at least as effective as ciprofloxacin at healing corneal ulcers infected with Pseudomonas aeruginosa when gatifloxacin is administered less frequently than ciprofloxacin. Trends favored gatifloxacin in fluorescein retention scores [2].Clinical indications: Bacterial infection FDA Approved Date: Toxicity: Hepatotoxicity; Acute pancreatitis [3]; Torsades de pointes [4]
Antibacterial agent 134 (compound 1) is an diketopiperazine alkaloid with antimicrobial activity. Antibacterial agent 134 is the major metabolite in the culture of Hymeniacidon perleve associated bioactive bacterium Pseudomonas sp. NJ6-3-1[1].
D13-9001 is a potent AcrB (AcrAB-TolC efflux pump subunit) and MexB (MexAB-OprM efflux pump subunit) inhibitor with the KD values of 1.15 μM and 3.57 μM in E. coli and P. aeruginosa, respectively[1]. D13-9001 exhibits antibiotic activities[2].
Anti-Trypanosoma cruzi agent-5 (compoung 8) is a potent inhibitor of Trypanosoma cruzi proliferation[1].
Dolutegravir sodium is an inhibitor of HIV-1 integrase-catalyzed strand transfer with IC50 of 2.7 nM.
Sulfaclozine is an efficacious sulphonamide derivative with antibacterial and anticoccidial effects.Target: Antibacterial, AntiparasiticSulfaclozine is an antibiotic commonly used in poultry for the treatment of coccidiosis and various infectious diseases, in broiler chickens. Sulfaclozine is commonly used for the treatment of various poultry diseases (particularly, collibacteriosis, fowl cholera and coccidiosis).
Carindacillin (Carbenicillin indanyl) sodium is an orally active and broad-spectrum antimicrobial agent. Carindacillin sodium can be hydrolyzed to Carbenicillin in vivo. Carindacillin sodium can be used for the research of urinary-tract infection[1][2].
(+)-Epieudesmin is an antineoplastic agent. (+)-Epieudesmin has marginal cancer cell line inhibitory activities. (+)-Epieudesmin inhibits the growth of Gram-negative pathogen[1].
7-Methyl-DL-tryptophan (7-Methyltryptophan) is an amino acid derivative, which is a key precursor for biosynthesis of many non-ribosomal peptide antibiotics. 7-Methyl-DL-tryptophan plays an important role in synthesis of high-efficiency antibacterial agents and analogues thereof[1].
Tellimagrandin II (Eugeniin), the first intermediate in the 4C1-glucose derived series of ellagitannins, also inhibits antibiotic resistance of drug-resistant Staphylococcus aureus[1][2].
STING agonist-22 (CF501) is a potent non-nucleotide STING agonist. STING agonist-22 is a adjuvant by activating STING to induce the type I interferon (IFN-I) response and proinflammatory cytokine production. STING agonist-22 can be used as an adjuvant to boost the original protein vaccine, producing potent, broad, and long-term immune protection. STING agonist-22 can be used for SARS-CoV-2 variants and sarbecovirus diseases research[1].
Verrucarin J (Muconomycin B) is a metabolite of the Myrothecium fungus family. Verrucarin J generates reactive oxygen species (ROS) and induces apoptosis of cancer cell lines, such as A549, HCT 116 and SW-620 cells. Verrucarin J shows activities against Candida albicans and Mucor miehei. Verrucarin J inhibits arenavirus Junin (JUNV) yield with an IC50 of 1.2 ng/mL[1][2][3][4][5].
Cys-TAT(47-57) (Cys-[HIV-Tat (47-57)]) is an arginine rich cell penetrating peptide derived from the HIV-1 transactivating protein.