GNF179 metabolite is the metabolite of GNF179, which is an optimized 8,8-dimethyl IP analog that exhibited the potency(4.8 nM against the multidrug resistant strain W2) in vitro metabolic stability and in vivo oral bioavailability.IC50 value: Target: Anti-parasitic agentGNF179 exhibits a low clearance (CL=22 ml/min/kg, ~25% of hepatic blood flow in mice), a large volume of distribution (steady-state volume of distribution, Vss=11.8 l/kg), a moderate residence time (MRT=9 hours) and suitable terminal half-life (t1/2=8.9 hours). GNF179 reduced Plasmodium berghei parasitemia levels by 99.7% with a single 100 mg/kg oral dose, and prolonged mouse survival by an average of 19 days. GNF179 was able to protect against an infectious P. berghei sporozoite challenge with a single oral dose at 15 mg/kg while NITD609 was not.
Acetyl-Adhesin (1025-1044) amide is a 20-peptide fragment of Streptococcus pyogenes cell surface adhesin that acts as an antimicrobial peptide to specifically inhibit the binding of adhesin to salivary receptors and prevent recolonization of Streptococcus pyogenes[1].
Tirandamycin A, an antibiotic, is a bacterial RNA polymerase inhibitor. Tirandamycin A has antiamoebic and antibacterial properties[1][2].
Anti-infective agent 2 (compound 3k) shows antiparasitic activity against P. falciparum and T. brucei rhodesiense, with IC50 values of 0.07 and 2.20 μM, respectively. Anti-infective agent 2 shows antimycobacterial activity against Mycobacterium smegmatis with a MIC of 32 μg/mL[1].
Albendazole sulfone is a metabolite of Albendazole, and exhibits anti-parasite effect against Echinococcus multilocularis Metacestodes[1][2].
(E)-3,4-Dimethoxycinnamyl alcohol is an antimutagenic. (E)-3,4-Dimethoxycinnamyl alcohol has antimutagenic activity against furylfuramide, Trp-P-1, and activated Trp-P-1[1].
Antibacterial agent 154 (compound 7) is a derivative of Fluoroqinolones and is an orally effective antibacterial agent. Antibacterial agent 154 inhibits Gram-positive and Gram-negative bacteria. Antibacterial agent 154 demonstrated in vivo efficacy in a mouse model of staphylococcal sepsis[1].
Cecropin A (1-7)-Melittin A (2-9) is an antimicrobial peptide with antimicrobial activity against a broad spectrum of Gram-positive and Gram-negative aerobic bacteria, as well as antimalarial activity, without the adverse hemolytic properties of bee venom peptides[1].
Colistin is a polypeptide antibiotic which inhibits gram-negative bacteria by binding to lipopolysaccharides and phospholipids in the outer cell membrane of gram-negative bacteria.
Triflumezopyrim, a mesoionic insecticide, has high efficiency at a low dosage, and is mainly used to control hopper species. Triflumezopyrim mainly acts on the nicotinic acetylcholine receptor (nAChR) inhibition, which is very highly 44 efficient, rapidly effective, and nearly nontoxic to nontarget arthropods[1].
IMP-1088 is a potent, selective human N-myristoyltransferase with IC50 of less than 1 nM for both HsNMT1 and HsNMT2, inhibits Rhinoviruses (RVs) capsid myristoylation in cells; pharmacological and rapidly inhibits host-cell N-myristoylation, potently and efficiently block RV replication (IC50=17 nM) without cytotoxicity; potently blocks a key step in viral capsid assembly, to deliver a low nanomolar antiviral activity against multiple RV strains, poliovirus and foot and-mouth disease virus, and protection of cells against virus-induced killing.
R-10015, a broad-spectrum antiviral compound for HIV infection, acts as a potent and selective inhibitor of LIM domain kinase (LIMK) and binds to the ATP-binding pocket, with an IC50 of 38 nM for human LIMK1[1].
Sulfametrole is an orally active and potent antibacterial. Sulfametrole can be used for infections research, such as HIV, severe pneumonia and UTIs (urinary tract infections)[1][2].
Heliomicin is an antimicrobial peptide from Heliothis Virescens[1].
Peretinoin is an oral acyclic retinoid, inhibits HCV RNA amplification and virus release by altering lipid metabolism.Target: HCVin vitro: Peretinoin is an acyclic retinoid, improves the hepatic gene signature of chronic hepatitis C following curative therapy of hepatocellular carcinoma. Peretinoin is an oral acyclic retinoid with a vitamin A-like structure that targets retinoid nuclear receptors, such as retinoid X receptor and retinoic acid receptor. Peretinoin inhibits HCV RNA amplification and virus release by altering lipid metabolism. Peretinoin suppresses the RNA replication of H77S.3/GLuc2A most efficiently and its EC50 was 9 μM. Peretinoin may reduce the recurrence of hepatocellular carcinoma (HCC) following surgical ablation of primary tumours. Peretinoin inhibits RNA replication for all genotypes and showed the strongest antiviral effect among the retinoids tested. in vivo: In addition, Peretinoin prevents the development of hepatoma in several different hepatoma models.
Triclopyricarb (SYP-7017) is a strobilurin fungicide that can be used in crops disease control. Triclopyricarb inhibits mycelial growth with EC50 values ranged from 0.006 µg/mL to 0.047 µg/mL[1][2].
Bruceine J, a quassinoid, is a nature product that could be isolated from fruits of Br. jaVanica. Bruceine J has anti-Babesial activity[1].
Clinafloxacin(PD-127391) is a fluoroquinolone antibiotic.Target: AntibacterialClinafloxacin is a broad-spectrum antibiotic of the quinolone carboxylic acid category currently in development for intravenous and oral therapy of serious infections [1]. Clinafloxacin is a novel fluoroquinolone with potent broad-spectrum in vitro activity against gram-positive, gram-negative, and anaerobic pathogens. Clinafloxacin is highly active against S. pneumoniae 7785 (MIC, 0.125 μg/mL), and neither gyrA nor parC quinolone resistance mutations alone have much effect on this activity [2]. Clinafloxacin is identified as the most active fluoroquinolone against S. pneumoniae when compared with ofloxacin, levofloxacin, sparfloxacin, grepafloxacin, and trovafloxacin and is currently being evaluated as an antipneumococcal agent [3].
LMW peptide is an antimicrobial peptide. LMW peptide is active against Gram-positive and Gram-negative bacterial, such as B. subtilis, L. monocytogenes, E. coli, P. aeruginosa, V. cholera[1].
TMC647055 is a potent nonnucleoside NS5B polymerase inhibitor of HCV replication. TMC647055 has potent HCV combine activity with an IC50 value of 82 nM. TMC647055 can be used for the research of Hepatitis C virus (HCV)[1][2].
Bacampicillin is a penicillin antibiotic, is a prodrug of ampicillin with improved oral bioavailability.
Nithiamide is a non-5-nitroimidazole drugs, is a antibiotic used in veterinary.
Bis-propargyl-PEG5 is a PEG-based PROTAC linker used in the synthesis of PROTACs. Bis-propargyl-PEG5 is used for the synthesis of carbohydrate receptors (SCRs) with anti-Zika activity[1].
Caspofungin-d4 (MK-0991-d4; L-743872-d4) is a deuterium labeled Caspofungin (HY-17006A). Caspofungin is a potent antifungal agent. Caspofungin inhibits the synthesis of the fungal cell wall component β-(l,3)-D-glucan[1][2][3].
Zika virus-IN-1 (Compd 2) is a Zika virus inhibitor, with an EC50 of 1.56 μM [1].
Arylomycin A2, an Antibiotic (Antibiotic), is a lipopeptide type I signal peptidase (SPase I) inhibitor. Arylomycin A2 has antibacterial effects[1].
β-Yohimbine (Amsonin) is an indole alkaloid that can be isolated from Aspidosperma ulei Markgr. β-Yohimbine shows antiplasmodial activity against the Chloroquine (HY-17589A)-resistant Fc M29-Cameroon strain (IC50: > 1 μg/mL)[1].
Bulevirtide (Myrcludex B) is a NTCP inhibitor, a linear lipopeptide of 47 amino acids. Bulevirtide inhibits HBV and HDV entry into liver cells, blocks HBV infection in hepatocytes, and participates in HBV transcriptional suppression. Bulevirtide can be used in HDV infection and compensated cirrhosis research[1][2].
Lobendazole is a potent anthelmintic. Lobendazole inhibits Giardia intestinalis strains[1].
Sofosbuvir impurity K, an diastereoisomer of sofosbuvir, is the impurity of sofosbuvir. Sofosbuvir (PSI-7977) is an inhibitor of HCV RNA replication, demonstrates potent anti-hepatitis C virus activity.