SARS-CoV-2-IN-20 (Compound 1a) is a potent inhibitor of SARS-CoV-2 with an EC50 of 6.5 μM. SARS-CoV-2-IN-20 has the potential for the research of infection diseases[1].
Cosfroviximab (c13C6-FR1) is a mouse/human chimeric monoclonal antibody against Ebola virus glycoprotein (EBOV-GP)[1].
HBV-IN-15 is a potent inhibitor of covalently closed circular DNA (cccDNA). cccDNA serves as the template for viral RNA transcription and subsequent viral DNA generation. HBV-IN-15 is a flavone derivative. HBV-IN-16 has the potential for the research of HBV infection (extracted from patent WO2020052774A1, compound 2)[1].
LYS228 is a novel potent monobactam that shows potent activity against carbapenem-resistant isolates of Enterobacteriaceae with MIC90 of 2 ug/ml; LYS228 is stable against Metallo-β-lactamases (MBLs), and shows small or no MIC shifts for most SBLs (serine β-lactamases), including CTX-Ms, KPCs and OXA-types. Bacterial Infection Phase 2 Clinical
Ticarcillin is a semisynthetic, extended-spectrum, carboxypenicillin antibacterial agent, and is active against gram-positive cocci, including streptococci and staphylococci. Ticarcillin is also effective against most gram-negative organisms, including Pseudomonas aeruginosa. Ticarcillin can be used in lower respiratory tract infections, skin and skin structure infections, urinary tract infections, and intraabdominal infections research[1][2][3].
EBOV/MARV-IN-3 (compound 32) is a potent EBOV and MARV inhibitor with IC50 values of 0.5, 1.2 µM, respectively. EBOV/MARV-IN-3 binds to the hydrophobic pocket close to EBOV Y517. EBOV/MARV-IN-3 shows antiviral activity[1].
α-Vitamin E-d9 is the deuterium labeled α-Vitamin E[1]. α-Vitamin E ((+)-α-Tocopherol), a naturally occurring vitamin E form, is a potent antioxidant[2][3].
Hesperetin 7-O-glucoside is produced by the enzymatic conversion of Hesperidin. Hesperetin 7-O-glucoside is a potent human HMG-CoA reductase inhibitor and also effectively inhibits the growth of Helicobacter pylori. Antihypertensive effect[1][2].
Comanthoside B is a flavonoid glycoside isolated from the aerial portions of Ruellia tuberosa L. Comanthoside B has anti-inflammatory and antiseptic activities[1].
Pyrazinamide-d3 is deuterium labeled Pyrazinamide. Pyrazinamide (Pyrazinecarboxamide; Pyrazinoic acid amide) is a potent and orally active antitubercular antibiotic. Pyrazinamide is a prodrug that is converted to the active form pyrazinoic acid (POA) by PZase/nicotinamidase encoded by the pncA gene in M. tuberculosis[1][2].
1233B is a secondary metabolite from filamentous fungus, Fusarium sp. RK97-94[1].
Aureothricin is a dithiolopyrrolone (DTP) antibiotic first isolated from Streptomyces and exhibits relatively broad-spectrum antibiotic activity. Aureothricin can inhibit adhesion of human umbilical vein endothelial cells (HUVECs) to vitronectin[1].
AN11251 is a potent and oral active anti-Wolbachia agent with potential for treatment of onchocerciasis and lymphatic filariasis, with EC50 values of 1.5 nM in LDW1 cell lines and 15 nM in C6/36 cell lines[1].
Daunorubicin (Daunomycin) citrate is a topoisomerase II inhibitor with potent anti-tumor activity. Daunorubicin citrate inhibits DNA and RNA synthesis. Daunorubicin citrate is a cytotoxin that inhibits cancer cell viability and induces apoptosis and necrosis. Daunorubicin citrate is also an anthracycline antibiotic. Daunorubicin citrate can be used in the research of infection and variety of cancers, including leukemia, non-Hodgkin lymphomas, Ewing's sarcoma, Wilms' tumor[1][2][4][5].
Mecarbinate is an anti-hepatitis C virus (HCV) agent.
Apelin-36(human) is an endogenous orphan G protein-coupled receptor APJ agonist, with an EC50 of 20 nM. Apelin-36(human) shows high affinity to human APJ receptors expressed in HEK 293 cells (pIC50=8.61). Apelin-36 has been linked to two major types of biological activities: cardiovascular and metabolic. Apelin-36(human) inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ[1][2][3][4].
Oxynitidine is an HBV inhibitor (ID50=30.8 µg/mL), which can effectively inhibit the DNA replication activity of HBV. Oxynitidine can be used in the study of viral infections[1].
Triticonazole is a triazole pesticide. Triticonazole an azole fungicide, shows endocrine disrupting activities[1][2].
Kansuinine B inhibits IL-6-induced Stat3 activation. Kansuinine B possesses anti-viral activity and could be used in the study for COVID-19[1][2][3].
Erythromycin-d3 is the deuterium labeled Erythromycin[1]. Erythromycin is a macrolide antibiotic produced by actinomycete?Streptomyces erythreus?with a broad spectrum of antimicrobial activity. Erythromycin binds to bacterial 50S ribosomal subunits and inhibits?RNA-dependent protein synthesis?by blockage of transpeptidation and/or translocation reactions, without affecting synthesis of nucleic acid. Erythromycin also exhibits antitumor and neuroprotective effect in different fields of research[2][3][4][5].
VNRX-5133 is a cyclic boronate β-lactamase inhibitor. VNRX-5133 has direct inhibitory activity against serine-active site β-lactamases (Ser-BL) and metallo-β-lactamases (MBL). VNRX-5133 is highly active against multidrug-resistant (MDR)-K. pneumonia and P. aeruginosa clinical isolates[1].
Danoprevir is a NS3/4A protease inhibitor for hepatitis C virus (HCV) with IC50 of 0.2-3.5 nM. The inhibition effect on HCV genotypes 1A/1B/4/5/6 is approximately 10-fold higher than 2B/3A.
RSV-IN-5 (Compound 4) is a potent dual inhibitor of wild-type and mutant respiratory syncytial virus (RSV) fusion proteins. RSV-IN-5 exhibits potent anti-RSV activities against not only wild-type A2 F protein (EC50=2.0 nM), but also D486N-mutant F protein (EC50=8.1 nM)[1].
Sulfanitran-d4 is the deuterium labeled Sulfanitran. Sulfanitran is an antibacterial and anticoccidial agent used in poultry feeds. Sulfanitran also is a multidrug resistance protein 2 (MRP2) stimulator that can increase the affinity of MRP2 for estradiol-17-β-D-glucuronide (E217βG)[1][2].
Antibacterial agent 38 is an antibacterial agent extracted from patent WO2015063714A1, compound C. Antibacterial agent 38 can be used for the research of bacterial infections[1].
Valifenalate(IR5885; Valiphenal), which is approved for application on high-value crops such as grapes, tomatoes and other vegetables, is effective against various types of mildew and is currently marketed primarily under the Valis moniker; insecticide agent.
PLpro/RBD-IN-1 (compound 5) is a dual SARS-CoV-2 PLpro and spike protein RBD inhibitor with IC50s of 7.197 μM and 8.673 μM, respectively[1].
Amantadine-d6 is the deuterium labeled Amantadine[1]. Amantadine (1-Adamantanamine) is an orally avtive and potent antiviral agent with activity against influenza A viruses. Amantadine inhibits several ion channels such as NMDA and M2, and also inhibits Coronavirus ion channels. Amantadine also has anti-orthopoxvirus and anticancer activity. Amantadine can be used for Parkinson's disease, postoperative cognitive dysfunction (POCD) and COVID-19 research[2][3][4][5][6][7].
Cyclo(L-Leu-L-Pro) is an inhibitory substance targeting to production of norsolorinic acid (NA,a precursor of aflatoxin),which can be isolated from A. xylosoxidans NFRI-A1. Cyclo(L-Leu-L-Pro) inhibits accumulation of NA by A. parasiticus NFRI-95 and inhibits spore formation. Cyclo(L-Leu-L-Pro) inhibits aflatoxin production with an IC50 of 0.2 mg/mL in A. parasiticus SYS-4[1].