2-Phenylethanol-d9 is the deuterium labeled 2-Phenylethanol[1]. 2-Phenylethanol (Phenethyl alcohol), extracted from rose, carnation, hyacinth, Aleppo pine, orange blossom and other organisms, is a colourless liquid. It has a pleasant floral odor and also an autoantibiotic produced by the fungus Candida albicans[2]. It is used as an additive in cigarettes and also used as a preservative in soaps due to its stability in basic conditions.
Methyl Paraben-13C6 (Methyl 4-hydroxybenzoate-13C6) is a 13C labeled Methyl Paraben (HY-N0349)[1]. Methyl Paraben, isolated from the barks of Tsuga dumosa the methyl ester of p-hydroxybenzoic acid, is a standardized chemical allergen. Methyl Paraben is a stable, non-volatile compound used as an antimicrobial preservative in foods, agents and cosmetics. The physiologic effect of Methyl Paraben is by means of increased histamine release, and cell-mediated immunity[2].
Clevudine is an antiviral drug for the treatment of hepatitis B. Target: HBVClevudine is a nucleoside analog with an unnatural beta-L configuration. Clevudine showed potent antiviral activity during therapy and induced a sustained posttreatment antiviral effect for 6 months after a 12-week treatment period, and this was associated with a sustained normalization of ALT levels [1]. Clevudine showed a potent antiviral response, and its effect was higher in HBeAg-negative patients, with rapid viral load reduction after therapy. However, long-term therapy for more than 1 year resulted in the development of considerable resistance and myopathy. Therefore, we should consider alternative antiviral agents if clevudine resistance or clevudine-induced myopathy is developed in patients on clevudine for the treatment of CHB [2].
Antibacterial agent 42, an antibacterial agent, significantly lowers MIC value of antibacterial agent Ceftazidime[1].
AMOZ-d5 is a deuterium labeled AMOZ. AMOZ, a tissue bound metabolite of Furaltadone, Furaltadone is a synthetic nitrofuran antibiotic widely used[1].
Odesivimab is a humanized monoclonal antibody, targeting Ebola virus glycoprotein with a KD value of 7.74 nM for recombinant histidine-tagged Makona strain Ebola virus glycoprotein ectodomain protein. Odesivimab can be used in research of Ebola virus infection[1].
Ornidazole(Ro 7-0207) is a 5-nitroimidazole derivative with antiprotozoal and antibacterial properties against anaerobic bacteria. Target: Antibacterial; AntiparasiticOrnidazole is a drug that cures some protozoan infections. Ornidazole 1 g/day is effective for the prevention of recurrence of Crohn's disease after ileocolonic resection [1]. Ornidazole is converted to reduction products that interact with DNA to cause destruction of helical DNA structure and strand leading to a protein synthesis inhibition and cell death in susceptible organisms [2].
Chloroorienticin A (A82846B) is a glycopeptide antibiotic. Chloroorienticin A exhibits excellent activity against staphylococci and streptococci[1].
Camalexin is a phytoalexin isolated from Camelina sativa and Arabidopsis (Cruciferae) with antibacterial, antifungal, antiproliferative and anticancer activities. Camalexin can induce reactive oxygen species (ROS) production[1][2][3].
Ac-D-DGla-LI-Cha-C is a potent HCV protease inhibitor peptide. Ac-D-DGla-LI-Cha-C can be used for the research of cancer, autoimmune diseases, fibrotic diseases, inflammatory diseases, neurodegenerative diseases, infectious diseases, lung diseases, heart and vascular diseases and metabolic diseases[1].
Pyrimethanil is an anilinopyrimidine and broad-spectrum contact fungicide for the control of Botrytis spp. on a wide variety of crops[1]. Pyrimethanil inhibits the biosynthesis of methionine and other amino acids in Botrytis cinerea. Pyrimethanil can be used for the research of fungal diseases prevention on fruit, vegetable and ornamental plants with mold infection[3].
Cap-dependent endonuclease-IN-20 is a cap-dependent endonuclease (CEN) inhibitor. Cap-dependent endonuclease-IN-20 shows antiviral activity against influenza virus A/Hanfang/359/95 (H3N2) with IC50 of 4.82 μM (CN112940009A; DSC801)[1].
Epinodosin is a diterpenoid. Epinodosin has moderate cytotoxicity against HL-60 cells with IC50 value of 10.4 μM. Epinodosin can be used for the research of inflammatory diseases[1].
Alstonine is a major indole alkaloid compound of a plant-based remedy. Alstonine has antipsychotic, anxiolytic, anticancer and antimalarial properties[1].
Paritaprevir (ABT-450) dihydrate is a potent, orally active and antiviral non-structural protein 3/4A (NS3/4A) protease inhibitor with EC50s of 1 and 0.21 nM against HCV 1a and 1b, respectively. Paritaprevir dihydrate is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.31 μM. Paritaprevir dihydrate is metabolized primarily by cytochrome P450 (CYP) 3A. The plasma concentration and half-life of Paritaprevir dihydrate can be enhanced by Ritonavir (a CYP450 inhibitor)[1][2][3][4].
Telavancin (TD-6424) is a semisynthetic lipoglycopeptide vancomycin-derivative, is a novel antimicrobial agent developed by Theravance for overcoming resistant Gram-positive bacterial infections, specifically methicillin-resistant Staphylococcus aureus (MRSA). Telavancin disrupts cell membrane integrity, can be used for research of complicated skin and skin structure infections (cSSSIs) caused by Gram-positive bacteria[1].
Mtb-IN-4 (compound 17h) is a nontoxic isoxazole, with anti-Mycobacterium tuberculosis (Mtb) activity (IC50=0.70 μM). Mtb-IN-4 inhibits Mtb respiration and biofilm formation in macrophage, and enhances antibiotic isoniazid (INH) inhibition against INH-resistant Mtb mutant[1].
Galidesivir triphosphate (Immucillin-A triphosphate) is converted by the prodrug Galidesivir. Galidesivir triphosphate is a substrate for viral RNA-dependent RNA polymerase (RDRP), resulting in termination of viral RNA replication and thus serves as an antiviral. Galidesivir triphosphate inhibits HCV NS5B RNA polymerase activity and protects mice against Ebola[1][2].
Dinotefuran is an insecticide of the neonicotinoid class, its mechanism of action involves disruption of the insect's nervous system by inhibiting nicotinic acetylcholine receptors.Target: nAChR, Antiparasitic
Antitubercular agent-27 (compound 1) is a potent antitubercular agent with an IC50 value of 3.2 µM, an MIC value of 7.8 µM, an IC90 value of 7.0 µM. Antitubercular agent-27 shows antimycobacterial activity for resistant isolates of Mycobacterium tuberculosis H37Rv. Antitubercular agent-27 shows effective intracellular antimycobacterial activity and low cytotoxicity[1].
10-10-Hydroxyaloin A is potent SARS-CoV-2 inhibitor. 10-Hydroxyaloin A exhibits significant efficacy to bind SARS-Cov-2 Mpro active site[1].
Urease-IN-7 (Compound 5k) is a competitive Urease inhibitor (IC50: 3.33 μM, Ki: 3.62 μM). Urease-IN-7 can be used for research of peptic and gastric ulcers[1].
Sordarin is a potent diphthamide-dependent eEF2 inhibitor with antifungal properties. Sordarin targets eEF2 so as to inhibit protein translation by blocking eEF2-mediated translocation of tRNAs. Sordarin inhibits translation specifically in certain fungi (e.g. C. albicans, C. glabrata, and C. neoformans) while unable to do so in some other fungal species (e.g. Candida parapsilosis and Candida lusitaniae)[1][2].
Cefoselis is a widely used beta-lactam antibiotic.Target: AntibacterialCefoselis, a new parenteral cephalosporin, was active against clinical isolates of both gram-positive and gram-negative aerobic bacteria. The activity of Cefoselis was similar to that of cefpirome and cefepime and generally superior to that of ceftazidime. Cefoselis showed potent antibacterial activity against Hemophilus influenzae and Moraxella catarrhalis.Cefoselis was highly active against MSSA and MSCNS. Cefoselis was poor in the activity against MRSA,MRCNS,PRSP and Enterococcus faecalis,and no activity for Enterococcus faecium.
4,5-Dichlorocatechol is a substrate of the broad-spectrum chlorocatechol 1,2-dioxygenase of pseudomonas chlororaphis RW71. The Ki values for 4,5-dichlorocatechol is 30 nM for the dioxygenase of the Chlorobenzoate-degrading strain Pseudomonas putida AC27 and 4 nM for the dioxygenase of Acidovorax sp. strain PS14[1].
Antiviral agent 30 (Example 118) is an antiviral agent. Antiviral agent 30 is active against HCV and RSV (IC50: > 25μM)[1].
Retrocyclin-1 is a kind of Theta-defensin. Retrocyclin-1 recognizes and binds to carbohydrate-containing surface molecules, to protect cells from HIV-1 infection. Retrocyclin-1 exhibits high affinity to fetuin, gp120 (Kd=35.4 nM), CD4 (Kd=31 nM), and galactosylceramide (Kd=24.1 nM)[1].
Ceftaroline fosamil hydrate acetate is a potent cephalosporin antibiotic. Ceftaroline fosamil hydrate acetate shows broad-spectrum activity against Gram-positive pathogens, including methicillin-resistant Staphylococcus aureus (MRSA) and multidrug-resistant Streptococcus pneumoniae, and common Gram-negative organisms. Ceftaroline fosamil hydrate acetate has anti-infective activity, and can be used for the research of complicated skin and skin structure infections (cSSSIs) and community-acquired bacterial pneumonia (CABP)[1][2][3].
Gomisin M1 ((±)-Gomisin M1) is a potent anti-HIV agent with an EC50 of <0.65 μM[1].
Cyclophilin inhibitor 1 is a potent and orally bioavailable cyclophilin A inhibitor, with a Kd of 5 nM, shows effective anti-HCV activity, with an EC50 of 98 nM for HCV 2a[1].