Antivirals

Boceprevir is a peptidomimetic, covalent inhibitor of NS3/4A serine protease from hepatitis C virus (HCV). Boceprevir also inhibits and acts as a substrate in the cytochrome P450 3A4 (CYP3A) metabolic pathway. Boceprevir was recently shown to inhibit the main protease Mpro (3CLpro) from SARS-CoV-2 with IC50 of 4.13 μM and EC50 of 1.31 μM.

Stability Very Hygroscopic Applications Tenofovir Dimer is a dimer of Tenofovir (T018500). Tenofovir is a reverse transcriptase inhibitor. Used as an anti-HIV agent. References Shaw, J.-P., et al.: Pharm. Res., 14, 1824 (1997), Wyles, D., et al.: Clin Infect. Dis., 40, 174 (2005), Peng, J., et al.: J. Clin. Pharmacol., 46, 265 (2006), Seminari, E., et al.: J. Antimicrob. Chemother., 60, 831 (2007),

2,2'-Anhydrouridine (2,2'-Cyclouridine) is a research tool for antiviral and anticancer studies.

Stearyl glycyrrhetinate boosts antiviral activity, reduces inflammation, and suppresses allergies in pharma and cosmetics.

Vicriviroc is an investigational pharmaceutical compound, specifically classified as an HIV entry inhibitor. It originates from a synthetic source, designed to target the CCR5 co-receptor on human immune cells. The mode of action involves blocking this co-receptor, thereby preventing the HIV virus from binding and fusing with the host cell membrane. This inhibition effectively obstructs the virus's ability to enter and infect the host cells, particularly those within the chemokine receptor family. Vicriviroc's primary use is as a potential antiretroviral agent in the treatment of HIV-1 infection. Its application focuses on patients whose strains of HIV predominantly use the CCR5 receptor for cellular entry. By interfering with the virus's entry mechanism, Vicriviroc aims to reduce viral load and impede disease progression. Although it has shown promise in clinical trials, ongoing research and development continue to evaluate its efficacy and safety in comparison to existing therapeutic options.

Norwogonin (5,7,8-Trihydroxyflavone), isolated from Scutellaria baicalensis Georgi, possesses antiviral activity against Enterovirus 71 (IC50: 31.83 μg/ml).

Epirengynic acid has antiviral activity against RSV

Daclatasvir dihydrochloride is an oral antiviral that treats chronic hepatitis C by inhibiting HCV's NS5A; rare liver enzyme elevation, seldom causes jaundice.

Viramidine is a nucleotide analogue prodrug, which is derived from naturally occurring nucleosides, specifically optimized for enhanced therapeutic profiles. Its mode of action involves conversion into ribavirin triphosphate within the body. This active form inhibits viral RNA polymerase, a critical enzyme necessary for viral replication. By disrupting the synthesis of viral RNA, Viramidine effectively reduces viral proliferation within host cells. Primarily, Viramidine is investigated and utilized in the context of antiviral treatments, especially for hepatitis C virus (HCV). It serves as an alternative to ribavirin, aiming to maintain efficacy while reducing the associated hemolytic anemia observed in ribavirin use. Viramidine's design allows for targeted liver delivery, enhancing its antiviral effectiveness and minimizing systemic exposure. The research focus on Viramidine highlights its potential in improving the therapeutic index of conventional ribavirin by offering a more hepatic-selective approach. Scientists continue to explore its pharmacokinetics and dynamics to optimize clinical outcomes in antiviral regimens.

IQP-0528: Potent NNRTI, blocks HIV entry, microbicidal gel, EC50: 0.2 nM for HIV-1, 100 nM for HIV-2.

Applications An intermediate for the preparation of Lamivudine and Emtricitabine. References Chang, C., et al.: J. Biol. Chem., 267, 13938 (1992), Jeong, L., et al.: J. Med. Chem., 36, 181 (1993).

Applications (S)-Tenofovir is an S-enatiomeric derivative of Tenofovir (T018500). (S)-Tenofovir displays virucidal activity against herpes, visna virus and retrovirus. The S enantiomer of Tenofovir (T018500) is less effective against HIV than their (R)-enantiomeric counterparts. References Balzarini, J. et al: Biochem. Biophys. Res. Comm., 219, 337 (1996); Balzarini, J. et al.: Antimicrob. Agents. Ch., 37, 332 (1993); Thormar, H. et al.: Antimicorb. Agents. Ch., 37, 2540 (1993)

Robinetin (3,3',4',5',7-Pentahydroxyflavone) has antioxidant and antiradical activities, inhibits EYPC membrane lipid peroxidation and HbA glycosylation with

Applications An adamantane derivative used in the preparation of organosilicon compounds with antiviral activity. Memantine impurity C. References Grishina, E.V. et al.: Khim.-Farmat. Zhur., 22, 315 (1988);

Amitivir (LY 217896)-an IMP dehydrogenase inhibitor that blocks MDCK cell division and may increase uric acid without affecting flu A.

Abacavir is an antiviral nucleoside reverse transcriptase inhibitor that is used for the treatment of HIV. This drug inhibits the activity of HIV-1 reverse transcriptase (RT) both by competing with dGTP and by its incorporation into viral DNA. Abacavir is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready to use products for assay development, screening or other R&D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.

Impurity Atazanavir Impurity B Applications An intermediate for the preparation of antiviral protease inhibitors. Atazanavir Impurity B References Fassler, A., et al.: J. Med. Chem., 39, 3203 (1996), Bold, G., et al.: J. Med. Chem., 41, 3387 (1998).

Bonafton (Bonaphthone) is an antiviral agent.

Applications An intermediate used in the preparation of Zanamivir derivatives. References Andrews, D., et al.: Eur. J. Med. Chem., 34, 563 (1999), Altamore, T., et al.: Bioorg. Med. Chem., 14, 1126 (2006),

N-Benzoyl-(2R,3S)-3-phenylisoserine (taxol side chain) is an intermediate in the preparation of potent anticancer drug Paclitaxel, used to study the location of

(-)-Arctigenin ((-)-Arctigenin) is found in burdock.

1. Epigoitrin (Goitrin) has anti-virus activity. 2. Epigoitrin has anti-oxidant activity. 3. Epigoitrin has anti-inflammation activity.

3'-Azido-3'-deoxy-5-methylcytidine inhibits HIV-1 reverse transcriptase(EC50 = 0.06 μM) and is an effective inhibitor of xenotropic murine leukemia-related

Applications 5,6,7,8-Tetrahydro-1-naphthalenol was used as a reagent in the synthesis of phosphonamidate and phosphonodiamidate prodrugs of adefovir and tenofovir which are used in the treatment of HIV infections. Also used in the synthesis of tetrahydronaphthalene-1-ol derivatives which were found to be promising potent antitumor agents. References Pertusati, F., et al.: Eur. J. Med. Chem., 78, 259 (2014); Dong, Y., et al.: Bioorg. Med. Chem. Lett., 19, 6289 (2009);

Selective and potent inhibitor of sialidases (neuraminidases) in influenza A and B viruses. The compound binds tightly to the viral neuraminidase active site in late stages of viral life-cycle. It inhibits shedding sialic acids from host cell surface glycans, which interact with viral hemagglutinin, and consequently prevents release of new viral particles from the host cell surface.

Sodium Camptothecin: plant-derived, antitumor, inhibits RNA/DNA synthesis, disrupts viral DNA.

Indinavir monohydrate is an antiretroviral medication, which is a synthetic pharmaceutical compound, specifically a protease inhibitor, used in the treatment of HIV infection. It is derived from chemical synthesis processes that follow rigorous standards to produce a pharmacologically active compound. Indinavir functions by selectively inhibiting the HIV-1 protease enzyme, which is crucial for the viral replication cycle. By binding to the active site of the enzyme, indinavir prevents the cleavage of viral polypeptides, leading to the production of immature and non-infectious viral particles. The primary use of indinavir monohydrate is in highly active antiretroviral therapy (HAART) regimens, often in combination with other antiretroviral agents, to effectively reduce viral load and increase CD4 cell counts in patients infected with HIV-1. This contributes to delaying the progression of the disease to AIDS and improving the quality and duration of life in affected individuals. Its application extends to both initial and salvage therapy in the management of HIV, providing a critical component in the arsenal of pharmaceutical interventions against the virus.

Applications Cabotegravir O-β-D-Glucuronide is a metabolite of Cabotegravir (C050100), a long acting HIV-1 integrase inhibitor with action against a broad range of HIV subtypes. References Yoshinaga, T. et al.: Antimicrob, Agents Chemother., 59, 397 (2015); Andrews, C. et al.: Sci. Transl. Med., 7, 270 (2015)

IND24 has anti-prion activity and can be used to study neurodegenerative diseases.

BVDV-IN-1 is a non-nucleoside inhibitor (NNI) of bovine viral diarrhea virus (BVDV), with an EC50 of 1.8 μM.

Applications Picornavirus replication inhibitor. Antiviral. Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package References Kearns, G.L., J. Clin. Pharmacol., 39, 613 (1999), Schmidtke, M. et al.: Antiviral Res. 81, 56 (2009)

Applications Intermediate in the production of Oseltamivir. It is a COVID19-related research product. References Kim, C., et al.: J. Med. Chem., 41, 2451 (1998), Carbain, B., et al.: Chem. Med. Chem., 4, 335 (2009),

Inarigivir ammonium, an antiviral dinucleotide, lowers HBV DNA and activates innate immunity via RIG-I agonism.

Dihydromollugin is a naphthol ester found in Rubia cordifolia that may have anti-tumour, virus-inhibiting and other activities.

Bemnifosbuvir (AT-511) is a novel phosphoramidate prodrug of 2'-fluoro-2'-C-methylguanosine-5'-monophosphate that has potent in vitro activity against HCV.

DL-Serine is a non-essential amino acid and a natural ligand and allosteric activator of pyruvate kinase M2.

Antiviral agent 17, EC50 0.015 μM in human assay, effective against murine norovirus, may aid infectious/malignant disease research.

Inhibitor of viral neuraminidase enzyme, effective against influenza A and B viruses. This antiviral compound inhibits neuraminidase-mediated cleavage of host cell sialic acids, which interact with newly synthesised virions from the host cell. This prevents virion budding from the host, resulting in inhibition of virion release and viral infection overall.