Antivirals

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.

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.

Penciclovir is an antiviral agent and acyclic guanine derivative that has proven efficient in the treatment of Herpes Simplex type 1 and 2 (HSV1 and HSV2) infection. Penciclovir is transformed by the virus into an active derivative able to block the deoxyguanosine triphosphate substrate binding site of the HSV polymerase.

Atazanavir is an antiviral protease inhibitor, used in the anti-retroviral therapy of adult and sometimes paediatric patients infected with HIV. This drug inhibits the processing of viral Gag and Gag-pol polyproteins in HIV-1 infected cells by binding to the HIV-1 protease active site.

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

Ritonavir is a HIV protease inhibitor. It has an anti-retroviral activity as it inhibits the protease enzymes specific of both HIV-1 and HIV-2 and has been shown to be effective in controlling virus replication in humans and animals. Ritonavir works by preventing the HIV viral protease enzyme from cleaving the structural and replicative proteins produced by HIV genes such as gag and pol.

Non-nucleoside reverse transcriptase inhibitor; antiviral agent against HIV

Tenofovir is an acyclic nucleoside phosphonate that exhibits anti-viral properties through its inhibition of reverse transcriptases. In particular, Tenofovir is a potent inhibitor of Human Immunodeficiency Virus (HIV) and chronic Hepatitis B Virus (HBV) reverse transcriptases, thus preventing the replication of genetic viral material. This property is beneficial in virus research areas and developing antiviral treatments. Once inside the body tenofovir is metabolized into its active form, tenofovir diphosphate, by the lysosomal protease cathepsin A, nucleotide kinases and adenylate kinases. 
Tenofovir 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.

Anti-viral; inhibitor of cytomegalovirus-terminase complex

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.

Ganciclovir is an acyclovir analog that is used in the treatment of cytomegalovirus and herpetic keratitis of the eye. This drug is a DNA polymerase inhibitor and exhibits its anti-viral properties by inhibiting viral replication.

N-Boc-protected -Guanidino Oseltamivir is a fine chemical that belongs to the group of versatile building blocks. It is a complex compound that has been used in research as a reagent and speciality chemical. N-Boc-protected -Guanidino Oseltamivir is an important intermediate for the synthesis of a variety of useful compounds, such as pharmaceuticals and natural products. This compound is also used as a reaction component in organic syntheses, especially for the preparation of high quality and useful scaffolds.

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

Applications 1-[2-O-(Phenoxythioxomethyl)-3,5-O-[1,1,3,3-tetrakis(1-methylethyl)-1,3-disiloxanediyl]-β-D-ribofuranosyl]-1H-1,2,4-triazole-3-carboxamide is an intermediate in the synthesis of 2’-Deoxyribavirin-5’-triphosphate (D2149940) Triethylamine Salt, a potential new inhibitor for HIV-1 replication.
References Vivet-Boudou, V., et al.: Nucleos. Nucleot. Nucl., 26, 743 (2007);

Applications Intermediate in the preparation of Ribavirin.

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 α-Ribavirin.

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

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

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 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),

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 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)

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);

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 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 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)

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

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 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);

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.

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.

RNA polymerase (RdRp) inhibitor

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.

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.

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.

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

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

Epetirimod (S-30563) is a small molecule immunomodulator with antitumor and anti-infective activity for the study of papillomavirus infections.