Antivirali

Rupintrivir is a peptidomimetic antiviral with action on rhinovirus 3C protease to inhibit viral replication and is used for research on rhinovirus and other viral infections.

Nucleoside analog with antiviral activity against coronaviruses, hepatitis and influenzas viruses. EIDD 1931 inhibited the Middle East Respiratory Syndrome coronavirus (MERS-CoV) and the murine hepatitis virus (MHV) replication in vitro at submicromolar concentrations. EIDD 1931 is able to evade the proofreading exonuclease ExoN and presents with high barrier to development of drug resistance.

Darunavir is a HIV-1 protease inhibitor used orally in the treatment of patients with multi-drug resistant HIV-1 infection (Ghosh, 2007). It has also been shown to be effective against other infectious diseases such as hepatitis C virus and SARS coronavirus. Metabolized by cytochrome P450 3A (CYP3A) isoenzymes, darunavir is often administered together with ritonavir that prolongs its bioavaiability, giving a terminal elimination half-life (t1/2) of 15 hours (Back, 2008). The effect of darunavir on natural compounds such as matrix proteins and toll-like receptor activity has also been studied via high performance liquid chromatography (HPLC) experiments.

Inhibitor of hepatitis C viral enzyme NS3-4A serine protease

Saquinavir is a HIV protease inhibitor drug that is used with other antiretroviral drugs for the treatment of HIV-1. As this drug prevents HIV protease activity, it prevents the proteolysis of the Gag polyprotein and thus results in non-infectious virus particles.

Darunavir is a HIV-1 protease inhibitor used orally in the treatment of patients with multi-drug resistant HIV-1 infection (Ghosh, 2007). It has also been shown to be effective against other infectious diseases such as hepatitis C virus and SARS coronavirus. Metabolized by cytochrome P450 3A (CYP3A) isoenzymes, darunavir is often administered together with ritonavir that prolongs its bioavaiability, giving a terminal elimination half-life (t1/2) of 15 hours (Back, 2008). The effect of darunavir on natural compounds such as matrix proteins and toll-like receptor activity has also been studied via high performance liquid chromatography (HPLC) experiments.

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.

Raltegravir is an antiretroviral agent used for the treatment of HIV infections in conjunction with other antiretrovirals. It inhibits the activity of HIV-1 integrase, which impedes the insertion of HIV-1 DNA into the host cell genome. Raltegravir also inhibits resistant mutants of HIV-1 that are associated with disease activity and progression.

Anti-viral; inhibits Hepatitis C virus NS3/4a protease

Filociclovir is a novel antiviral agent, which is synthesized from small-molecule pharmaceutical compounds. It functions primarily by inhibiting viral DNA polymerase, thereby halting viral replication within infected host cells. This mechanism of action is particularly effective against certain herpesviruses, as it targets the polymerase enzyme that is critical for viral DNA synthesis and proliferation.

Applications (R)-(((1-(6-Amino-9H-purin-9-yl)propan-2-yl)oxy)methyl)phosphonic Acid Methyl Ester Trimethylamine is an intermediate in the synthesis of Tenofovir (T018500), is an acyclic phosphonate nucleotide analogue.
References Peng, J., et al.: J. Clin. Pharmacol., 46, 265 (2006), Seminari, E., et al.: J. Antimicrob. Chemother., 60, 831 (2007),

Applications Intermediate in the preparation of α-Ribavirin.

Applications 2-Hydroxy-2-methylpropanethioamide is an thioamide compound integrated as an constituent in the synthesis of Ritonavir (R535000) and its derivatives.

Applications A highly reactive thiol-specific spin-label. A specific conformational probe of thiol site structure by virtue of its minimal rotational freedom and distance from the covalent disulfide linkage to the macromolecule under study.

Applications Intermediate in the preparation of Ribavirin.

Applications Used in the synthesis of enantioselective synthesis of carbocyclic ribavirin, its analogs and other antiviral agents.
References Kuang, R. et al.; Tetrahedron Lett. 41, 9575 (2000)

Applications (S)-2-(3-((2-(2-Hydroxypropan-2-yl)thiazol-4-yl)methyl)-3-methylureido)-3-methylbutanoic Acid is an intermediate in the synthesis of Ritonavir (R535000) derivatives.

Applications T-705RMP TEA Salt is a metabolite of T-705RMP (CAS# 356783-08-9), which is a reagent used for the preparation of pyrazine-ribofuranose derivatives as antiviral agents that are useful in the treatment of viral infections. T-705 (Favipiravir) [F103350] gets converted to T-705RMP by host cells, but T-705RMP has little inhibitory effect on the replication of the host cells based on biological studies.
References Zhong, B., et al.: Faming Zhuanli Shenqing, 2014:924257 (2014); Yousuke, F., et al.: Antimicrob Agent Chemother., 49, 981 (2005)

Applications Levovirin is a monocyclic L-nucleosides with type 1 cytokine-inducing activity. Levovirin is the L-enantiomer of Ribavirin (R414475) with similar immunomodulatory activity but does not have direct antiviral activity or hemolytic anemia.
References Ramasamy, K.S. et al.: J. Med. Chem., 43, 1019 (2000); Fang, C. et al.: J. Appl. Toxicol., 23, 453 (2003):

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);

Applications R 77975 is used to modulate lipophilicity in human rhinovirus capsid binders. It also is used in order to identify potential ativiral agents.
References Morley, A. et al.: Bioorg. Med. Chem. Lett., 21, 6031 (2011); Tomkinson, N. et al.: Bioorg. Med. Chem. Lett., 22, 7494 (2012);

Applications 2'-Fluoro-2'-deoxyuridine-5,6-d2 (CAS# 362049-50-1) is a useful isotopically labeled research compound.

Stability Hygroscopic
Applications (2'R)​-2'-​Deoxy-​2'-​fluoro-​2'-​methyl-uridine 5'-​Triphosphate Tetrasodium Salt is an impurity of Sofosbuvir (P839640) which is a prodrug that is metabolized to the active antiviral agent 2'-deoxy-2'-α-fluoro-β-C-methyluridine-5'-monophosphate.
References Lam, A.M.,et al.: Antimicrob. Agents. Chemotherapy., 56, 3359 (2012); Lam, A.M., et al.: J. Virol., 85, 12334 (2011); Sofia, M.J., et al.: J. Medn. Chem., 53, 7202 (2010);

Applications Darunavir intermediate.
References Ghosh, A., et al.: J. Med. Chem., 39, 3278 (1996), Ghosh, A., et al.: Bioorg. Med. Chem. Lett., 1998, 8, 687 (1998), Richman, D., et al.: Nature, 410, 995 (2001), Koh, Y., et al.: Antimicrob. Agents Chemother., 47, 3123 (2003),

Applications 2-Fluoro-3-methoxyaniline is a reagent that is used in the structure-activity relationship studies on a series of cyclopentane-containing macrocyclic inhibitors of hepatitis C virus NS3/4A protease leading to the discovery of TMC435350.
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 Raboisson, R., et al.: Bioorg. Med. Chem. Lett., 18, 4853 (2008)

Impurity Nelfinavir Sulphone Impurity
Applications Nelfinavir Sulfone is an impurity of Nelfinavir Mesylate (N389750). It is a COVID19-related research product.
References Aymard, G., et al.: J. Chromatogr. B, 744, 227 (2000), Jing, Q., et al.: J. Pharm. Biomed. Anal., 41, 1065 (2006),

Applications A model compound for studies of binding of influenza virus hemaglutinin and metal ions.
References Sauter, N.K., et al.: Biochemistry, 28, 8388 (1989), Sharon, N., et al.: Science, 246, 227 (1989), Nagy, J.O., et al.: J. Med. Chem., 35 (23), (1992), Knibbs, R.N., et al.: J. Biol. Chem., 268 (25), 18524 (1993)

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).

Applications Stavudine-alpha,alpha,alpha,6-d4 (CAS# 1219803-67-4) is a useful isotopically labeled research compound.

Applications 3,4-Difluoroaniline-2,6-d2 (CAS# 1061566-62-8) can be used in its derivative form as an antiviral agent for Hepatitis B.
References Qiu, Y.L., et.al., U.S. Pat. Appl. Publ., 187,(2019);

Applications Darunavir intermediate.
References Ghosh, A., et al.: J. Med. Chem., 39, 3278 (1996), Ghosh, A., et al.: Bioorg. Med. Chem. Lett., 1998, 8, 687 (1998), Richman, D., et al.: Nature, 410, 995 (2001), Koh, Y., et al.: Antimicrob. Agents Chemother., 47, 3123 (2003),

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),

Impurity Atazanavir Impurity (Pyridinyl Benzaldehyde)
Applications Reactive metabolite of atazanavir. Atazanavir Impurity; Pyridinyl Benzaldehyde impurity
References F. Li et al., Drug Metabolism and Disposition 39, 294 (2011)

Applications An intermediate in the synthesis of Ritonavir.
References Sham, H., et al.: Bioorg. Med. Chem. Lett., 12, 3101 (2002),

Lobucavir is an antiviral compound with a mode of action that inhibits viral DNA polymerase. It is used for treating infections caused by herpesviruses and hepatitis B virus.

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.

RNA polymerase (RdRp) inhibitor

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.

Sofosbuvir is an antiviral agent that is used for the treatment of hepatitis C infections and is used in combination with other antiviral agents. This drug is an inhibitor of viral RNA polymerase called non-structural protein 5B (NS5B). As a result, it inhibits viral RNA replication.

Foscarnet sodium is a pyrophosphate analog antiviral agent with action on viral DNA polymerase and is used for treating cytomegalovirus and herpes simplex virus infections.

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

SARS-CoV-2 nsp13-IN-1 (C1) inhibits nsp13 ssDNA+ATPase (IC50: 6 μM), not ssDNA-ATPase; useful for COVID-19 research.