Galactofucan (Fucogalactan) is a sulfated polysaccharide. Galactofucan can be extracted from brown seaweed Saccharina longicruris with anticoagulant, anti-tumor, anti-thrombosis, anti-inflammatory and antiviral properties. Galactofucan shows antiviral activities to HSV-1 and HSV-2 with IC50s of 0.76 and 1.34 µg/mL, respectively. Galactofucan can be used for the research of cancer and inflammation[1][2].
Thiocillin I is a thiopeptide antibiotic and has in vitro antibacterial activity against Gram-positive bacterial strains. The MIC values of Thiocillin I against S. aureus 1974149, E. faecalis 1674621, B. subtilis ATCC 6633 and S. pyogenes 1744264 are 2 μg/mL, 0.5 μg/mL, 4 μg/mL and 0.5 μg/mL, respectively[1].
β-Lactamase-IN-7 (compound 14) is a potent VIM-Type metallo-β-lactamase inhibitor, with Kis of 1.26 μM and 0.54 μM for VIM-1 and VIM-4, respectively. β-Lactamase-IN-7 can effectively inhibit Klebsiella pneumoniae[1].
Cephaloridine is a broad-spectrum antibacterial antibiotic. Cephaloridine has certain dose-related nephrotoxicity[1][2].
Teicoplanin is a semisynthetic glycopeptide antibiotic used in the prophylaxis and treatment of serious infections caused by Gram-positive bacteria, including Methicillin-resistant Staphylococcus aureus and Enterococcus faecalis.
Moenomycin complex is a potent transglycosylase inhibitor. Moenomycin complex inhibits bacterial growth by blocking the transglycosylase activity of class A penicillin-binding proteins (PBPs)[1].
Antifungal agent 33 (compound 4e) is a potent antifungal agent. Antifungal agent 33 exhibits remarkable antifungal activity against C. albicans, with a MIC of 16 μg/mL. Antifungal agent 33 shows potent inhibitory activity against Lanosterol 14α-demethylase (CYP51), with an IC50 of 0.19 μg/mL[1].
Cabotegravir is a potent HIV integrase inhibitor as an oral lead-in tablet and long-acting injectable for the treatment and prevention of HIV infection. Cabotegravir is an inhibitor of OAT1 (IC50 0.81 μM) and OAT3 (IC50 0.41 μM).IC50 value: 0.81 μM (OAT1), 0.41 μM (OAT3) [1]Target: OAT1, OAT3Cabotegravir is a potent HIV integrase inhibitor in clinical development as an oral lead-in tablet and long-acting injectable for the treatment and prevention of HIV infection.[2] Cabotegravir is an HIV-1 integrase inhibitor under development as a tablet for both oral lead-in therapy and long-acting (LA) injectable for intramuscular dosing.[3]
Azvudine (RO-0622) hydrochloride is a potent nucleoside reverse transcriptase inhibitor (NRTI), with antiviral activity on HIV, HBV and HCV. Azvudine hydrochloride exerts highly potent inhibition on HIV-1 (EC50s ranging from 0.03 to 6.92 nM) and HIV-2 (EC50s ranging from 0.018 to 0.025 nM). Azvudine hydrochloride inhibits NRTI-resistant viral strains[1].
OYYF-175, an antimicrobial antifolate, is a dihydrofolate reductase (DHFR) inhibitor with an IC50 of 2.36 nM for Escherichia coli DHFR. OYYF-175 exhibits potent broad-
GW433908 is a phosphate ester prodrug of the antiretroviral protease inhibitor amprenavir, with improved solubility over the parent molecule and a potential for reduced pill burden on current dosing regimens; GW433908G is the calcium salt of the prodrug.IC50 Value:Target: HIV Proteasein vitro: There were no significant changes in buprenorphine or PI plasma levels and no significant changes in medication adverse effects or opioid withdrawal. Increased concentrations of the inactive metabolite buprenorphine-3-glucuronide suggested that darunavir-ritonavir and fosamprenavir-ritonavir induced glucuronidation of buprenorphine[1].in vivo: Fosamprenavir-ritonavir administered with methadone did not alter plasma amprenavir pharmacokinetics compared with historical control data; nor did it alter the unbound R-methadone at 2 and 6 hours after methadone dosing. Pharmacodynamic indexes remained essentially unchanged after adding fosamprenavir-ritonavir to methadone [2]. After a high-fat meal compared with fasting, (1) the bioavailability of GW433908G suspension was decreased by 20% and Cmax by 41%, and (2) for GW433908G tablets, there was no influence on AUC(12% lower Cmax). After a low-fat meal compared with fasting, (1) there was bioequivalence for GW433908G tablets, but (2) bioavailability was decreased by 23% for amprenavir capsules (Cmax was also lower, by 46%) [3].Clinical trial: Study of an Investigational Regimen Including FDA Approved HIV Drugs In HIV-Infected Pediatric Subjects. Phase 2
Maximin 5 is an antimicrobial peptide derived from skin secretions of Bombina maxima. Maximin 5 has cytotoxicity on tumor cells and spermicidal effect[1].
Atazanavir-d6 is deuterium labeled Atazanavir. Atazanavir (BMS-232632), a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration[1]. Atazanavir (BMS-232632) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp)[2]. Atazanavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 3.49 μM[3].
10-Undecenoic acid was used as a starting reagent in the syntheses of Pheromone (11Z)-hexadecenal.
Piromidic Acid-d5 is the deuterium labeled Piromidic acid. Piromidic acid is an antibacterial agent. Piromidic acid is active against gramnegative bacteria and staphylococci and can be used for the research of intestinal, urinary, and biliary tract infections[1][2].
Nepetoidin B, an anti-inflammatory agent, inhibits inflammation by modulating the NF-κB and Nrf2/HO-1 signaling pathways. Nepetoidin B also has antifungal and antibacterial activity. Nepetoidin B is a natural product that can be obtained from Salvia plebeia R. Br. Nepetoidin B can be used in anti-inflammatory and anti-infectious research[1][2].
Anti-MRSA agent 3 (compound 18) has highly inhibitory activity against Methicillin-resistant Staphylococcus aureus (MRSA) with MIC of 0.098 μg/ml, and low cytotoxicity in normal cells. Anti-MRSA agent 3 has relatively strong ability to destroy bacterial cell wall and membrane, high binding affinity to bacterial genomic DNA[1].
Suvratoxumab (MEDI4893) is a long-acting, high-affinity humanized anti-α-toxin monoclonal antibody (IgG1κ type). Suvratoxumab potently neutralizes α-toxin, a key S. aureus virulence factor. Suvratoxumab improves survival and reduces lung injury in an immunocompromised mice model of pneumonia. Suvratoxumab also enhances the antibacterial activity of Vancomycin (HY-B0671) or Linezolid (HY-10394)[1][2][3].
Cephradine monohydrate (Cefradine monohydrate) is a first generation cephalosporin, which is active against a wide range of Gram positive and Gram-negative bacteria[1].
N-Acetylneuraminic acid-13C-2 is the 13C labeled N-Acetylneuraminic acid.
Chamaejasmenin D is an antimitotic and antifungal agent[1].
TMC353121 is a potent respiratory syncytial virus (RSV) fusion inhibitor with pEC50 of 9.9.
5-Bromo-5-nitro-1,3-dioxane, an antimicrobial compound, is effective against Gram-positive and Gram-negative bacteria and fungi, including yeast. 5-Bromo-5-nitro-1,3-dioxane inhibits enzyme activity and subsequent inhibition of microbial growth by the oxidation of essential protein thiol[1].
Mtb-cyt-bd oxidase-IN-2 is an inhibitor of Mycobacterium tuberculosis cytochrome bd oxidase (Mtb cyt-bd oxidase) with an IC50 value of 0.67 μM. Mtb-cyt-bd oxidase-IN-2 inhibits the growth of Mycobacterium tuberculosis with a MIC value of 256 μM. Mtb-cyt-bd oxidase-IN-2 can be used for the research of infection[1].
Tenofovir Disoproxil Fumarate is a nucleotide reverse transcriptase inhibitor to treat HIV and chronic Hepatitis B.
N-Phenylacrylamide is a special polymer showing high affinity with Ochratoxin A, a colorless and crystalline mycotoxin compound. N-Phenylacrylamide can be applied in the field of mycotoxin extraction, and be used for the security research of agricultural commodities and foods made from cereals and grapes[1].
3'-Azido-3'-deoxy-5-methylcytidine (CS-92) is a potent xenotropic murine leukemia-related retrovirus (XMRV) inhibitor with a CC50 of 43.5 μM in MCF-7 cells. 3'-Azido-3'-deoxy-5-methylcytidine also inhibits HIV-1 reverse transcriptase with an EC50 of 0.06 μM in peripheral blood mononuclear (PBM) cells[1].
ML303 is a pyrazolopyridine influenza virus nonstructural protein 1 (NS1) antagonist (IC90 = 155 nM), with an EC50 of 0.7 μM for Influenza A virus H1N1[1].
Cletoquine oxalate (Desethylhydroxychloroquine oxalate) is a major active metabolite of Hydroxychloroquine. Cletoquine oxalate is produced in the liver by CYP2D6, CYP3A4, CYP3A5, and CYP2C8 isoenzymes. Cletoquine oxalate is also a Chloroquine derivative and has the ability to against the chikungunya virus (CHIKV). Cletoquine oxalate has antimalarial effects and has the potential for autoimmune diseases treatment[1][2].
Siamycin I (BMY-29304), a 21-residue tricyclic peptide, is a secondary metabolite in actinomycetes. Siamycin I is a HIV fusion inhibitor with ED50s of 0.05 to 5.7 μM for acute HIV type 1 (HIV-1) and HIV-2 infections. Siamycin I inhibits the gelatinase and gelatinase biosynthesis-activating pheromone (GBAP) signaling via the FsrC-FsrA two-component regulatory system in a noncompetitive manner. Siamycin I suppresses the expression of both fsrBDC and gelE-sprE transcripts. Siamycin I, a lasso peptide, interacts with lipid II and inhibits cell wall biosynthesis. Siamycin I, an antibiotic, has the potential for enterococcal infections research[1][2][3][4].