Radalbuvir (GS-9669) is a non-nucleoside inhibitor of nonstructural protein 5B (NS5B) RNA-dependent RNA polymerase (RdRp). Radalbuvir shows strong anti-HCV potency (GT1a intrinsic EC50 = 2.9 nM, GT1b EC50 = 6 nM)[1].
Resiquimod-d5 (R848-d5) is deuterium labeled Resiquimod. Resiquimod is a Toll-like receptor 7 and 8 (TLR7/TLR8) agonist that induces the upregulation of cytokines such as TNF-α, IL-6 and IFN-α[1][2].
KIN101 is a potent RNA viral inhibitor with IC50s of 2 μM, >5 μM for influenza virus and Dengue virus (DNV), respectively. KIN101, an isoflavone agonist of IRF-3 dependent signaling, induces IRF-3 nuclear translocation. KIN101 has broad-spectrum activity against RNA viruses[1][2].
RO8191 (RO4948191), an imidazonaphthyridine compound, is an orally active and potent interferon (IFN) receptor agonist. RO8191 activates IFN-stimulated genes (ISGs) expression and JAK/STAT phosphorylation. RO8191 shows antiviral activity against both HCV and EMCV with an IC50 of 200 nM for HCV replicon[1].
Coblopasvir (KW136, KW-136) is a novel HCV NS5A inhibitor under development for treatment of HCV infection. HCV Infection Phase 3 Clinical
JTK-853 is a novel, non-nucleoside Hepatitis C Virus (HCV) polymerase inhibitor which shows effective antiviral activity in HCV replicon cells with EC50s of 0.38 and 0.035 µM in genotype 1a H77 and 1b Con1 strains, respectively.
Asunaprevir is a potent hepatitis C virus (HCV) NS3 protease inhibitor, with IC50 of 0.2 nM-3.5 nM.
Simeprevir (TMC435; TMC435350) sodium is an oral, potent and highly specific hepatitis C virus (HCV) NS3/4A protease inhibitor with a Ki of 0.36 nM. Simeprevir sodium inhibits HCV replication with an EC50 of 7.8 nM. Simeprevir sodium also potently suppresses SARS-CoV-2 replication and synergizes with Remdesivir. Simeprevir sodium inhibits the main protease (Mpro) and the RNA-dependent RNA polymerase (RdRp) of SARS-CoV-2, and also modulates host immune responses[1][4].
2'-C-Methyladenosine is an inhibitor of hepatitis C virus (HCV) replication. 2'-C-Methyladenosine inhibits HCV replicon and NS5B-catalyzed RNA synthesis with IC50 values of 0.3μM and 1.9 μM, respectively. 2'-C-Methyladenosine also potently inhibits LRV1 in Leishmania guyanensis (Lgy) and Leishmania braziliensis[1][2].
Deferiprone-d3 is the deuterium labeled Deferiprone. Deferiprone is the only orally active iron-chelating drug to be used therapeutically in conditions of transfusional iron overload[1][2].
Ombitasvir is a potent inhibitor of the hepatitis C virus protein NS5A, with EC50s of 0.82 to 19.3 pM against HCV genotypes 1 to 5, and 366 pM against genotype 6a.
HCV-IN-34 (compound 3i) is an orally active and potent HCV entry inhibitor. HCV-IN-35 shows excellent antiviral activity, with an EC50 of 0.010 μM and a CC50 (half-maximal cytotoxic concentration) of 8.23 μM[1].
Simeprevir is a potent HCV NS3/4A protease inhibitor which suppresses HCV replication with EC50 of 8 nM.
Platycodin D3 is a triterpenoid saponin isolated from Platycodon grandiflorum, with anti-HCV activity[1].
Astodrimer (SPL7013 free base) is a large (3-4 nm, ~ 16.5 kDa), negatively charged, highly-branched dendrimer, is a potent virucidal agent. Astodrimer shows antiviral and virucidal activity against a broad spectrum of viruses, including SARS-CoV-2, HIV-1, HSV-1, HSV-2, HPV. Astodrimer also has antibacterial properties[1][2][3].
Ledipasvir acetone is the active pharmaceutical ingredient of Ledipasvir. Ledipasvir is an inhibitor of the hepatitis C virus NS5A, with EC50 values of 34 pM against GT1a and 4 pM against GT1b replicon.
Azvudine (RO-0622) hydrochloride is a potent nucleoside reverse transcriptase inhibitor (NRTI), with antiviral activity on HIV, HBV and HCV. Azvudine hydrochloride exerts highly potent inhibition on HIV-1 (EC50s ranging from 0.03 to 6.92 nM) and HIV-2 (EC50s ranging from 0.018 to 0.025 nM). Azvudine hydrochloride inhibits NRTI-resistant viral strains[1].
Vaniprevir (MK-7009) is a non-covalent competitive inhibitor of the hepatitis C virus (HCV) NS3/4A protease.IC50 Value: Target: HCV NS3/4A Protease; HCVvaniprevir (MK-7009) is a macrocyclic hepatitis C virus NS3/4a protease inhibitor, is active against both the genotype 1 and genotype 2 NS3/4a protease enzymes. vaniprevir (MK-7009) has good plasma exposure and excellent liver exposure in multiple species.
PSI-6206 13CD3 is the deuterium labeled PSI-6206. PSI-6206 is the deaminated derivative of PSI-6130, which is a potent and selective inhibitor of HCV NS5B polymerase. PSI-6206 low potently inhibits HCV replicon with EC90 of >100 μM.
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.
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].
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.
Deapioplatycodin D is a triterpenoid saponin isolated from Platycodon grandiflorum, with anti-HCV activity[1].
Helioxanthin (ACH126447) and its analogues exhibit significant in vitro antiviral activity against hepatitis B virus (HBV, EC50=1 uM) and flavivirus.IC50 value: 1/3/2 uM (EC50, HBV/HCV/HSV-1) [1]Target: Anti-HBV; Anti flavivirusin vitro: Helioxanthin and its analogues decreased cellular RNA levels of HBV and antigen expression as well as selective inhibition of HBV replication in a cell culture model [2]. Helioxanthin analogue 8-1 exhibited anti-DHBV activity as demonstrated by quantification of viral DNA, RNA, covalently closed circular DNA and protein synthesis. Analogue 8-1 did not affect the stability of cellular macromolecules and did not have a sustained antiviral effect after drug removal. When DHBV replication was induced, virus-harbouring cells were more susceptible to the cytotoxicity of 8-1 than non-induced cells [3].
HCV-IN-7 hydrochloride is an orally active and potent pan-genotypic HCV NS5A inhibitor with IC50s of 3-47 pM. HCV-IN-7 hydrochloride shows a superior pan-genotypic profile and a good pharmacokinetic profile coupled with a favorable liver uptake. HCV-IN-7 hydrochloride has anti-viral activity[1].
Dehydrojuncusol, a potent HCV inhibitor, targets HCV NS5A and is able to inhibit RNA replication of replicons harboring resistance mutations to anti-NS5A direct-acting antivirals. Dehydrojuncusol significantly inhibits HCV infection when added after virus inoculation of HCV genotype 2a (EC50=1.35 µM)[1].
Mipomersen (ISIS 301012 free base) is an antisense oligonucleotide inhibitor of apolipoprotein B (apoB). Mipomersen has anti-HCV effect and reduces the infectivity of the HCV. Mipomersen can be used for the research of homozygous familial hypercholesterolemia (HoFH)[1][2].
4-Phenoxybenzylamine inhibits the function of the NS3 protein by stabilizing an inactive conformation with an IC50 of about 500 μM against FL NS3/4a.
PSI-353661 (GS-558093) is a purine nucleotide NS5B polymerase inhibitor against HCV infection (EC90: 8 nM). PSI-353661 can produce high concentrations of the active triphosphate in primary human hepatocytes[1][3].
HCV-IN-44 (compound 28) is an HCV NS5B protein inhibitor that can effectively inhibit the replication of HCV virus. HCV-IN-44 can be used for the study of HCV infection[1].