influenza a virus in 1

Influenza A virus-IN-1, a dihydropyrrolidones derivative, is a highly effective inhibitor of various subtypes of influenza A virus (IAV) with IC 50 values ranging from 3.11 μM to 7.13 μM. It effectively suppresses IAV replication and enhances the expression of key antiviral cytokines, such as IFN-β, and the antiviral protein MxA.

Influenza virus-IN-1 (compound 14) exhibits anti-influenza A virus activities which is a potent inhibitor of influenza A virus with an CC 50 of >200 μM and EC 50 of 2.46 μM. Influenza virus-IN-1 exhibits a concentration dependent inhibition activity for PAN endonuclease (EC 50 = 312.36 nM) [1].

CEF8, Influenza Virus NP (383-391) is an influenza A virus nucleoprotein containing residues 383 to 391, is the most important HLA-B*2705-restricted epitope in the nucleoprotein of influenza A viruses and is associated with escape from cytotoxic T lymphocytes-mediated immunity.HLA-B*3501 restricted influenza virus nucleoprotein epitope (383-391).

CEF27, Epstein-Barr Virus BRLF-1 lytic 148-156 acetate corresponding to amino acids 148-156 of the BRLF1. BRLF1 is a transcriptional activator that binds directly to a GC-rich motif present in some Epstein-Barr virus (EBV) lytic gene promoters.

Influenza A virus-IN-8 (S5), a macrocyclic peptide, exhibits no cytotoxicity and functions as a potent inhibitor of Influenza A Virus (IAV), demonstrating significant protease stability. It has IC50 values of 6.7 nM for H1 and 6.6 nM for H5 variants, indicating strong inhibitory effects. Furthermore, it has a high affinity for H1 variants, binding to a conserved region in the HA stem with a dissociation constant (Kd) of 1.0 nM [1].

Influenza A virus-IN-5 (Compound 16e) is a highly potent and orally active agent against the influenza A virus (IAV), exhibiting an IC 50 of 1.29 μM. It effectively inhibits the transcription and replication of viral RNA while maintaining acceptable levels of cytotoxicity [1].

Influenza virus-IN-2 (compound 19) has anti-influenza A virus activities that is a potent inhibitor of influenza virus with an CC 50 of 150.85 μM and EC 50 of 2.58 μM. Influenza virus-IN-2 concentration-dependently inhibits the PAN endonuclease with EC 50 of 489.39 nM [1].

Influenza A virus-IN-4 (compound 23b), a derivative of Oseltamivir, is a highly effective neuraminidase inhibitor. It exerts potent inhibitory effects on influenza viruses [1].

Influenza virus-IN-5 (Compound 5f) is an influenza virus hemagglutinin (HA) inhibitor that acts on the A/H3N2 virus (EC50: 1 nM).

Influenza virus-IN-6 (Compound 35) serves as a potent inhibitor targeting the N-terminal domain of the polymerase acidic protein (PA N ) endonuclease subunit of the influenza virus, exhibiting an inhibitory concentration 50 (IC 50 ) value of 0.20 μM [1].

Influenza virus-IN-7 (Example 16) is an orally active inhibitor of cap-dependent endonuclease, employed in research on influenza viral infectious diseases [1].

Influenza virus-IN-3 (compound 9) is a potent inhibitor of selective influenza viruses, acting on H5N1 (IC50: 0.88 μM), H5N2 (IC50: 0.10 μM), H5N6 (IC50: 5.5 μM), H5N8 (IC50: 0.51 μM). Influenza virus-IN-3 has antiviral and NA (neuraminidase) inhibitory effects and low cytotoxicity (CC50>200 μM).

Influenza A virus-IN-7 (compound 16r) is a potent, orally active inhibitor of influenza A virus (IC50: 3.43 μM, CC50>100 μM). Influenza A virus-IN-7 is an anti-IAV agent with low cytotoxicity and inhibits viral RNA transcription and replication.

HLA-A*0301-restricted epitope from Epstein-Barr Virus , EBV BRLF-1 (148-156).

Influenza A virus fragment has the RNA sequence of Leu-Lys-Phe-Ala-Phe-Ser-Met-Met.

Zika virus-IN-1 is an inhibitor of Zika virus (EC50: 1.56 μM).

Anti-virus agent 1 (compound 4i), a phosphoramidate prodrug of GS-5734, exhibits potent antiviral efficacy. It is primarily utilized in the study of coronavirus and Ebola virus (EBOV).

Influenza A virus-IN-6 (compound 16j) is a potent and selective inhibitor of influenza A virus （IC 50= 3.88 μM, CC50= 36.64 μM). Influenza A virus-IN-6 exhibits anti-IAV activity with low cytotoxicity.

Herpes Virus Inhibitor 1 is a compound that inhibits the replication of the herpes virus by disrupting the quaternary structure of its ribonucleotide reductase. This action effectively hinders the virus's ability to replicate [1] [2].

Partial antigenic glycoprotein

HLA-B*08 restricted influenza virus nucleoprotein epitope.

Influenza virus-IN-4 (compound 11e) is a potent inhibitor of influenza virus neuraminidase, acting on H5N1 (IC50: 3.4 μM), H5N2 (IC50: 0.094 μM), H5N6 (IC50: 0.79 μM) and H5N8 (IC50: 0.077 μM). Influenza virus-IN-4 inhibits NA (neuraminidase) and has low cytotoxicity (CC50 > 200 μM). influenza virus-IN-4 is not significantly toxic to mice at 1500 mg/kg.

Syncytial Virus Inhibitor-1 is a potent and orally bioavailable inhibitor of respiratory syncytial virus (RSV) fusion(EC50s of 0.002 μM, 0.004 μM, and 0.002 μM for RSV Long, RSV A2, and RSV B strains, respectively).

Influenza hemagglutinin is a type of hemagglutinin found on the surface of the influenza viruses. It is an antigenic glycoprotein. It is responsible for binding the virus to the cell that is being infected. Influenza hemagglutinin proteins bind to cells w

Molnupiravir (MK-4482) (EIDD-2801) is a prodrug of the ribonucleoside analog EIDD-1931 which is orally bioavailable. Molnupiravir can be used in COVID-19, seasonal and pandemic influenza research that has broad spectrum antiviral activity against multiple coronaviruses and influenza virus, for example, SARS-CoV-2, MERS-CoV, SARS-CoV [1][2].

1. Ginkgetin has anti-influenza virus and anti-fungal activities. 2. Ginkgetin has anti-inflammatory activity, can down-regulates COX-2 induction in vivo against skin inflammatory responses. 3. Ginkgetin is a good STAT3 inhibitor and may be a useful lead

Cap-dependent endonuclease-IN-1 is a highly potent and orally active cap-dependent endonuclease inhibitor with antiviral activity for the study of influenza virus infection.

Diridavumab, a monoclonal anti-HA stalk antibody, stabilizes the prefusion HA structure, thereby inhibiting the pH-dependent fusion of cellular and viral membranes in endosomes. This property renders it useful for research on H2 influenza virus [1].

Australine is a pyrrolizidine alkaloid originally isolated fromC. australethat has enzyme inhibitory activities.1,2,3It is an inhibitor of glucoamylase (IC50= 5.8 μM) that also inhibits glucosidase I, sucrase, maltase, andA. nigerα-glucosidase (IC50s = 20, 28, 35, and 28 μM, respectively).2,3Australine is selective for these enzymes over glucosidase II, α- and β-mannosidase, and α- and β-galactosidase up to 500 μM, β-glucosidase, with only 5% inhibition at 66 μM, as well as isomaltase and trehalase (IC50= 97 and 160 μM, respectively). Australine (500 μg/ml) inhibits glycoprotein processing of viral glycoproteins in influenza virus-infected MDCK cells and induces the accumulation of glycoproteins.2 1.Molyneux, R.J., Benson, M., Wong, R.Y., et al.Australine, a novel pyrrolizidine alkaloid glucosidase inhibitor from Castanospermum australJ. Nat. Prod.51(6)1198-1206(1988) 2.Tropea, J.E., Molyneux, R.J., Kaushal, G.P., et al.Australine, a pyrrolizidine alkaloid that inhibits amyloglucosidase and glycoprotein processingBiochemistry28(5)2027-2034(1989) 3.Kato, A., Kano, E., Adachi, I., et al.Australine and related alkaloids: easy structural confirmation by 13C NMR spectral data and biological activitiesTetrahedron Asymmetry14(3)325-331(2003)

Zanamivir-13C,15N2is intended for use as an internal standard for the quantification of zanamivir by GC- or LC-MS. Zanamivir is a sialic acid analog that inhibits neuraminidase release of newly replicated influenza virus particles.1It has been shown to selectively inhibit the growth of influenza A and B viruses in plaque reduction assays with IC50values ranging from 5 to 14 nM and to directly inhibit influenza A and B virus neuraminidases with IC50values ranging from 0.6 to 7.9 nMin vitro. Intranasal zanamivir administration at 0.4 mg/kg twice daily reduces mortality and viral titers in lung homogenates of mice infected with influenza. 1.Elliott, M.Zanamivir: From drug design to the clinicPhilos. Trans. R. Soc. Lond. B Biol Sci.356(1416)1885-1893(2001)

Ribavirin-13C5is intended for use as an internal standard for the quantification of ribavirin by GC- or LC-MS. Ribavirin is an antiviral guanosine nucleoside analog.1,2Upon entry into cells, ribavirin is metabolized to an active triphosphate form that induces viral RNA chain termination and inhibits viral polymerases. It reduces replication in a panel of seven RNA and four DNA viruses in Vero cells (EC50s = 2-95 μg/ml).3Ribavirin also reduces replication of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) in Vero cells (EC50= 109.5 μM).4Aerosol administration of ribavirin (30 mg/kg) reduces mortality in a mouse model of influenza A infection.5Formulations containing ribavirin have been used in the treatment of respiratory syncytial virus (RSV), hepatitis C virus (HCV), and viral hemorrhagic fevers. 1.Gilbert, B.E., and Knight, V.Biochemistry and clinical applications of ribavirinAntimicrob. Agents Chemother.30(2)201-205(1986) 2.Gordon, C.J., Tchesnokov, E.P., Woolner, E., et al.Remdesivir is a direct-acting antiviral that inhibits RNA-dependent RNA polymerase from severe acute respiratory syndrome coronavirus 2 with high potencyJ. Biol. Chem.295(20)6785-6797(2020) 3.Kirsi, J.J., North, J.A., McKernan, P.A., et al.Broad-spectrum antiviral activity of 2-β-D-ribofuranosylselenazole-4-carboxamide, a new antiviral agentAntimicrob. Agents Chemother.24(3)353-361(1983) 4.Wang, M., Cao, R., Zhang, L., et al.Remdesivir and chloroquine effectively inhibit the recently emerged novel coronavirus (2019-nCoV) in vitroCell Res.30(3)269-271(2020) 5.Wilson, S.Z., Knight, V., Wyde, P.R., et al.Amantadine and ribavirin aerosol treatment of influenza A and B infection in miceAntimicrob. Agents Chemother.17(4)642-648(1980)

10-Norparvulenone is a fungal metabolite originally isolated fromMicrosphaeropsis.1It decreases viral sialidase activity in, and increases survival of, MDCK cells infected with the mouse-adapted influenza virus A/PR/8/34 when used at a concentration of 1 μg/ml. 1.Fukami, A., Nakamura, T., Kim, Y.P., et al.A new anti-influenza virus antibiotic, 10-norparvulenone from Microsphaeropsis sp. FO-5050J. Antibiot. (Tokyo)53(10)1215-1218(2000)

Cap-dependent endonuclease-IN-9 is a potent (CEN) inhibitor with notable efficacy against the influenza virus and exhibits minimal cytotoxicity, enhanced in vivo pharmacokinetics, and robust pharmacodynamics. It effectively suppresses the RNA polymerase activity of A virus[1].

RSV-IN-3 (Compound 1) serves as a dual inhibitor targeting both the respiratory syncytial virus (RSV) and influenza virus A (IAV), demonstrating anti-RSV efficacy with an EC50 of 32.70 μM [1].

Defensin HNP-3 is a peptide secreted by human polymorphonuclear leukocytes (PMNs) that has antimicrobial properties. It induces lysis of mammalian cells when used at a concentration of 25 μg/mL. It also inhibits growth of E. faecalis (ED50 = 100 nM) and clinical isolates of P. aeruginosa (MIC90 = 4 μM). HNP-3 binds to recombinant HIV-1 envelope glycoprotein (gp120) and human CD4 (Kds = 52.8 and 34.9 nM, respectively). It also binds to recombinant, immobilized human surfactant protein D (SP-D; Kd = 55.7 nM) and inhibits focus formation in Madin-Darby canine kidney (MDCK) cells infected with influenza A virus (IAV).

Urumin, a compound with antiviral properties, inhibits human influenza A virus growth, particularly the PR8 strain, with an inhibitory concentration (IC 50) of 3.8 μM. It acts by targeting the conserved stalk of H1 hemagglutinin and can neutralize drug-resistant H1 influenza viruses. Additionally, Urumin offers protective effects against lethal influenza infection in naive mice [1].

HA-IN-1 (compound 5g), a high-affinity Hemagglutinin (HA) ligand, targets the trypsin cleavage site of HA to inhibit HA-mediated membrane fusion and decrease pulmonary virus titer in vivo. This compound emerges as a promising influenza A virus (IAV) inhibitor and anti-influenza agent [1].

Antiviral agent 35 (compound 4d) serves as a potent orally active inhibitor of the influenza virus, targeting early stages of viral replication. It suppresses influenza-induced ROS accumulation, autophagy, and apoptosis, along with the inflammatory response mediated by the RIG-1 pathway in a mouse model of pulmonary infection. Its cytotoxicity is minimal in MDCK cells, displaying a CC50 greater than 800 μM, and possesses anti-H1N1 (A/Weiss/43) activity with an EC50 of 2.28 μM [1].

Ketotifen (HC 20-511) is a second-generation, orally active noncompetitive histamine 1 (H1) receptor antagonist and mast cell stabilizer. It inhibits 6-phosphogluconate dehydrogenase (PGD) in vitro and displays antiviral activity against SARS-CoV-2 and the Influenza virus. Additionally, Ketotifen is utilized in researching autoimmune encephalomyelitis (EAE) and preventing asthma attacks.

Neuraminidase-IN-1 (Compound Y-1) is a novel neuraminidase inhibitor.

CAY10766 is an antiviral compound.1It inhibits entry of influenza virus-like particles pseudotyped with hemagglutinin A (HA) from H5N1 influenza A virus into A549 cells (EC50= 0.24 μM). CAY10766 (1 μM) reduces H1N1 and H5N1 influenza A viral titers in infected MDCK cells. It also exhibits synergy with oseltamivir carboxylate in MDCK cells infected with the influenza A reporter PR8-NS1-Gluc virus.

Colletodiol is a fungal metabolite that has been found inD. grovesiiand has immunosuppressant and antiviral activities.1,2It inhibits concanavalin A- or LPS-induced proliferation of isolated mouse splenocytes (IC50s = 12 and 5 μg/ml, respectively).1Colletodiol inhibits influenza A viral replication in HeLa-IAV-Luc cells.2 1.Fujimoto, H., Nagano, J., Yamaguchi, K., et al.Immunosuppressive components from an ascomycete, Diplogelasinospora grovesiChem. Pharm. Bull.46(3)423-429(1998) 2.Lai, W., Wang, S., and Ye, X.Colletodiol inhibits the replication of influenza A virus WSN/H1N1 by reducing the activity of viral RNA polymeraseWei Sheng Wu Xue Bao53(12)1334-1339(2013)

Gedivumab (MHAA4549A; RG7745), a human monoclonal antibody, exhibits high specificity in targeting the influenza A virus (IAV) by binding to the highly conserved stem region of the IAV hemagglutinin protein. This interaction inhibits hemagglutinin maturation and blocks hemagglutinin-mediated membrane fusion within the intranucleosome, making Gedivumab useful for studies on IAV infection disease [1].

KBC-007 is a synthetic branched chain-containing analog of α-galactosylceramide (α-GalCer). It induces IL-4 and IFN-γ secretion by mouse splenocytes when used at a concentration of 0.5 ng/ml and IL-2 secretion by DN32.D3 NKT hybridoma cells co-cultured with CD1d-transfected RBL cells pre-loaded with KBC-007 at a concentration of 8 ng/ml. KBC-007 (1 μg per animal) increases levels of IL-4, but not IFN-γ, to a similar degree as α-GalCer in mouse serum. KBC-007 (0.5 μg per animal) increases the survival rate of mice immunized with the inactivated influenza A virus A/PR/8/34 in a model of influenza infection.

Triton X-100 is a non-denaturing detergent that solubilizes lipid membranes. Triton X-100 is commonly used in laboratories and is applied to vaccines at different stages of the manufacturing process. Triton X-100 is listed as an excipient in certain vaccines including split virus influenza vaccines. Triton X-100 is a nonionic surfactant [1] [2].

Baloxavir-d4 is a deuterated compound of Baloxavir. Baloxavir has a CAS number of 1985605-59-1. Baloxavir is a first-in-class cap-dependent endonuclease inhibitor of the influenza virus polymerase PA subunit.

RSV-IN-4 (Compound 2) has anti-RSV activity with EC50 of 11.76 μM. RSV-IN-4 is a respiratory syncytial virus (RSV) and influenza virus A (IAV) dual inhibitor [1].

RdRP-IN-5 (compound 20), a potent inhibitor of the influenza virus RNA-dependent RNA polymerase (RdRP), has potential application in influenza research [1].

Viral polymerase-IN-1 hydrochloride, a derivative of Gemcitabine, effectively inhibits influenza A and B virus infections, demonstrating IC90 values ranging from 11.4 to 15.9 μM, and possesses activity against SARS-CoV-2 infection. This compound acts by interfering with viral RNA replication/transcription within cells [1].

Trimethoprim hydrochloride, a bacteriostatic antibiotic and dihydrofolate reductase inhibitor, demonstrates efficacy against a broad spectrum of Gram-positive and Gram-negative aerobic bacteria. It has research applications for urinary tract infections, Shigellosis, and Pneumocystis pneumonia. Additionally, when combined with zinc, it can inhibit the infection of Influenza A virus in chick embryos [1] [2] [3] [4].