HCV Protease

Hepatitis C virus (HCV)-specific protease inhibitors are a class of agents that block the enzymatic activity of the HCV NS3 protease region. HCV protease inhibitors, in combination with other antiviral drugs with anti-HCV activity (e.g., peginterferon, ribavirin, and the direct-acting drugs that block the NS5A and NS5B regions of the virus), result in a significant decrease in HCV replication. HCV NS3/4A protease is essential for viral multiprotein processing, RNA replication and virosome formation, and effectively cleaves and inactivates two important signaling molecules in the sensory pathway that react to HCV pathogen-associated molecular patterns (PAMPs) to induce interferons (IFNs).

HCV infection is associated with chronic liver disease, including hepatic steatosis, liver fibrosis, cirrhosis, and hepatocellular carcinoma. In recent years, the NS3-4A serine protease of HCV has been one of the most attractive targets for the development of specific antiviral drugs against HCV.

CAS No.	Product Name	Inquiry
1966138-53-3	Coblopasvir-dihydrochloride Coblopasvir (KW-136) dihydrochloride is a pangenotypic non-structural protein 5A (NS5A) inhibitor. Coblopasvir dihydrochloride can be used for research of chronic hepatitis C virus infection.
20831-76-9	Gentiopicroside Gentiopicroside is isolated from the roots of Gentiana manshurica Kitag.
2088243-03-0	NS5A-IN-4 NS5A-IN-4 (Compound 1.12) is an orally active pan-genotypic hepatitis C virus (HCV) NS5A inhibitor with IC50 values of 1.2, 2296, 4.6, 362, 10.3 and 693 pM against gT1b, gT1a, gT2a, gT3a, gT4a and gT5a.
208939-95-1	Hepatitis-Virus-C-NS3-Protease-Inhibitor-2 Hepatitis Virus C NS3 Protease Inhibitor 2 is a product-based peptide inhibitor of hepatitis C virus (HCV) NS3 protease, with a Ki of 41 nM.
2172676-02-5	Velpatasvir-[d7] Velpatasvir-[d7] is the labelled analogue of Velpatasvir, which is a selective Hepatitis C virus NS 5 protein inhibitor.
2750534-88-2	Faldaprevir-d6 Faldaprevir-d6 is deuterium labeled Faldaprevir.
300832-84-2	Ciluprevir Ciluprevir is used experimentally in the treatment of hepatitis C. It is manufactured by Boehringer Ingelheim Pharma GmbH & Co. kg and developed under the research code of BILN-2061. It is targeted against NS2-3 protease.
394730-60-0	Boceprevir An NS3 serine protease inhibitor of hepatitis C virus, for the treatment of HCV infection.
402957-28-2	Telaprevir Telaprevir is a potent, selective, peptidomimetic inhibitor of the hepatitis C virus (HCV) NS3-4A serine protease, and it demonstrated excellent antiviral activity both in genotype 1b HCV replicon cells (50% inhibitory concentration [IC50] = 354 nM) and in human fetal hepatocytes infected with genotype 1a HCV-positive patient sera (IC50 = 280 nM). Telaprevir forms a covalent but reversible complex with the genotype 1a HCV NS3-4A protease in a slow-on, slow-off process with a steady-state inhibition constant (K(i)*) of 7 nM. Dissociation of the covalent enzyme-inhibitor complex of Telaprevir and genotype 1a HCV protease has a half-life of almost an hour. A >4-log10 reduction in the HCV RNA levels was observed after a 2-week incubation of replicon cells with Telaprevir, with no rebound of viral RNA observed after withdrawal of the inhibitor. In several animal species, Telaprevir exhibits a favorable pharmacokinetic profile with high exposure in the liver. In a recently developed HCV protease mouse model, Telaprevir showed excellent inhibition of HCV NS3-4A protease activity in the liver.
50886-61-8	Isoeuphorbetin Isoeuphorbetin is a dimeric coumarin isolated from Viola philippica. Isoeuphorbetin is a potent inhibitor of HCV protease with an IC50 of 3.63 µg/mL.
640725-71-9	Valopicitabine dihydrochloride Valopicitabine dihydrochloride is a nucleoside analogue and the orally bioavailable 2'-C-methylcytidine (NM107) prodrug, with anti-hepatitis C virus (HCV) activity.
801283-95-4	Faldaprevir Faldaprevir, also called as BI 201335, is a potent, once-daily (QD), hepatitis C virus (HCV) NS3/4A protease inhibitor with the potential to treat HCV infection. Faldaprevir (BI 201335) is undergoing testing in a Phase II clinical study in Hepatitis C released by Trek Therapeutics.
817204-33-4	PSI-6130 PSI-6130 is a potent and selective inhibitor of HCV NS5B polymerase. It is metabolized to two pharmacologically active species in primary human hepatocytes.
849022-32-8	BI-1230 BI-1230 is potent and digit nanomolar inhibitor of HCV NS3 protease and of viral replication. BI-1230 is also highly selective against other serine/cysteine proteases. BI-1230 shows good Pharmacokinetic(PK) activity.
850876-88-9	Danoprevir Danoprevir(ITMN-191;R7227; RO5190591;RG7227) is a peptidomimetic inhibitor of the NS3/4A protease of hepatitis C virus (HCV) with IC50 of 0.2-3.5 nM, inhibition effect for HCV genotypes 1A/1B/4/5/6 is ~10-fold higher than 2B/3A.
865466-24-6	Narlaprevir Narlaprevir is a potent, selective, orally bioavailable inhibitor of the hepatitis C virus (HCV) nonstructural protein 3 serine protease that is primarily metabolized by the cytochrome P450-3A4 system.
877225-09-7	HCVP-IN-1 HCVP-IN-1 is an inhibitor of hepatitis C viral polymerase (HCVP).
923590-37-8	Vaniprevir Vaniprevir is a non-covalent competitive inhibitor of the hepatitis C virus (HCV) NS3/4A protease. It is a macrocyclic hepatitis C virus NS3/4a protease inhibitor, and is active against both the genotype 1 and genotype 2 NS3/4a protease enzymes. It has good plasma exposure and excellent liver exposure in multiple species.
929890-64-2	AZD-7295 AZD-7295 is a HCV NS5A protein inhibitor, with an EC50 of 7 nM for GT-1b replicon.
940908-79-2	R-7128 R-7128 is a selective nucleoside analog inhibitor of the hepatitis C virus (HCV) NS5B RNA-dependent RNA polymerase, with activity across all HCV genotypes. It is a nucleoside polymerase inhibitor (NPI) and is able to inhibit the RNA synthesis of HCV in vitro.

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