HCV Protease

CAS No.	Product Name	Inquiry
	NS5A-IN-1 NS5A-IN-1 is a prodrug of Pibrentasvir, an inhibitor of HCV NS5A.
	NS5A-IN-2 NS5A-IN-2 (Compound 33) is a potent inhibitor of NS5A. NS5A-IN-2 has extremely high potency against HCV genotype 1b, improved activity against genotype 3a (GT 3a) and good Metabolic stability.
	NS5A-IN-3 NS5A-IN-3 (Compound 15) is a potent inhibitor of NS5A. NS5A-IN-3 has extremely high potency against HCV genotype 1b, improved activity against genotype 3a (GT 3a) and good Metabolic stability. NS5A-IN-3 exhibits a higher resistance barrier than daclatasvir against genotype 1b.
	Simeprevir-13C-d3 Simeprevir-13C,d3 (TMC435-13C,d3) is the 13C- and deuterium labeled Simeprevir. Simeprevir is an oral, potent and highly specific hepatitis C virus (HCV) NS3/4A protease inhibitor with a Ki of 0.36 nM. Simeprevir inhibits HCV replication with an 50 of 7.8 nM. Simeprevir also potently suppresses SARS-CoV-2 replication and synergizes with Remdesivir. Simeprevir inhibits the main protease (Mpro) and the RNA-dependent RNA polymerase (RdRp) of SARS-CoV-2, and also modulates host immune responses.
	Telaprevir-d4 Telaprevir-d4 (VX-950-d4) is the deuterium labeled Telaprevir. Telaprevir (VX-950) is a highly selective, reversible, and potent peptidomimetic inhibitor of the HCV NS3-4A protease, the steady-state inhibitory constant (Ki) of Telaprevir is 7 nM against a genotype 1 (H strain) NS3 protease domain plus a NS4A cofactor peptide. Telaprevir inhibits SARS-CoV-2 3CLpro activity.
1001094-46-7	GS-9256
1036915-08-8	IDX184 IDX184 is a potent and orally bioavailable HCV replication inhibitor that potently inhibits HCV polymerase with an IC50 of 0.31 μM and a Ki of 52.3 nM.
1098189-15-1	Vedroprevir Vedroprevir is a selective hepatitis C virus (HCV) NS3 protease inhibitor. It is a pharmaceutical drug that is used in the treatment of hepatitis C virus in patients with HCV genotype 1(GT1) infection. It inhibits an important viral phosphoprotein, NS5A, which is involved in viral replication, assembly, and secretion. It retained wild-type activity against multiple classes of NS5B and NS5A inhibitor resistance mutations. It showed good oral bioavailability in all three species tested. It was developed by Gilead Sciences and was terminated in clinic phase 2 trials.
117824-04-1	Dehydrojuncusol 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).
1198784-72-3	BI-653048 BI 653048 is a selective and orally active nonsteroidal glucocorticoid (GC) agonist with an IC50 value of 55 nM. BI 653048 inhibits CP1A2, CYP2D6, CYP2C9, CYP2C19 and CYP3A4 isoforms' activity and reduces affinity for the hERG ion channel (IC50 >30 μM). BI 653048 is extracted from patent WO2005028501A1 (Compound 103), is also a HCV NS3 protease inhibitor that can reduce viral loads infected with the hepatitis C virus.
1198784-97-2	BI-653048-phosphate BI 653048 phosphate is a selective and orally active nonsteroidal glucocorticoid (GC) agonist with an IC50 value of 55 nM.
1200133-34-1	VCH-916 VCH-916 is a novel allosteric inhibitor of HCV NS5B polymerase. The RNA-dependent RNA polymerase (NS5B) of HCV is one of the attractive validated targets for development of new drugs to block HCV infection. VCH-916 is currently being evaluated for safety/tolerability, pharmacokinetics and anti-viral efficacy in chronically infected HCV patient.
1206524-86-8	MK-5172 potassium salt In biochemical assays, MK-5172 was effective against a panel of major genotypes and variants engineered with common resistant mutations observed in clinical studies with other NS3/4a protease inhibitors. In the replicon assay, MK-5172 demonstrated subnanomolar to low-nanomolar EC50s against genotypes 1a, 1b, and 2a. In rats, MK-5172 showed a plasma clearance of 28 ml/min/kg and plasma half-life of 1.4 hr. When dosed p.o. at 5 mg/kg, the plasma exposure of MK-5172 was good with an AUC of 0.7 uM.hr. The liver exposure of the compound was quite good (23 uM at 4 hr), and MK-5172 remained in liver 24 hr after a single p.o. 5 mg/kg dose. At 24 hr, the liver concentration of MK-5172 was 0.2 uM, which was over 25-fold higher than the IC50 in the replicon assay with 50% NHS. When dosed to dogs, MK-5172 showed low clearance of 5 ml/min/kg and a 3 hr half-life after i.v. 2 mg/kg dosing and had good plasma exposure (AUC=0.4 uM.hr) after a p.o. 1 mg/kg dose.
1241946-89-3	Simeprevir sodium salt Simeprevir is an orally bioavailable inhibitor of the hepatitis C virus (HCV) NS3/4A protease. It has been approved in combination with peginterferon-alfa and ribavirin for the treatment of HCV and HBV infections.
1009734-33-1	HZ-1157 HZ-1157 is an inhibitor of hepatitis C virus (HCV) nonstructural protein 3/4A (NS3/4A) protease.
630420-16-5	Asunaprevir Asunaprevir is a potent hepatitis C virus (HCV) non-structural protein protease inhibitor currently in Phase III clinical trials for the treatment of HCV infection.
1009119-65-6	Daclatasvir dihydrochloride Daclatasvir is a highly selective inhibitor of HCV NS5A with EC50 of 9-50 pM, for a broad range of HCV replicon genotypes and the JFH-1 genotype 2a infectious virus in cell culture.
1441674-54-9	Ledipasvir acetone Ledipasvir is an inhibitor of hepatitis C virus NS5A.
1350514-68-9	MK-5172 Grazoprevir is a hepatitis C virus protease inhibitor developed for the treatment of hepatitis C. It suppresses NS3 and NS4A, which play a role in the virus splitting its polyprotein into the functional virus proteins. Grazoprevir is often used in combination with elbasvir or ribavirin.
1377049-84-7	Velpatasvir Velpatasvir is a selective Hepatitis C virus NS 5 protein inhibitor originated by Gilead Sciences. It showed pan-genotypic activity and a high barrier to resistance in HCV replicon assays.

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