This document lists various compounds related to HCV protease inhibition and antiviral research.
1365970-03-1 C38H46F4N6O9S 838.87 glecaprevir targets viral protease mechanisms, blocking viral maturation, and is applied in antiviral drug research and development.
1422484-32-9 C46H56N8O8 848.99 GSK2818713 is a potent antiviral compound that inhibits key viral enzymes, interfering with viral replication, suitable for fundamental antiviral mechanism studies and early-stage drug discovery research.
1425038-27-2 C38H49N6NaO9S 788.89 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.
1456607-71-8 C40H47N7O9S 801.908 Paritaprevir (ABT-450) dihydrate is a potent, orally active and antiviral non-structural protein 3/4A (NS3/4A) protease inhibitor with EC50s of 1 and 0.21 nM against HCV 1a and 1b, respectively. Paritaprevir dihydrate is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.31 μM. Paritaprevir dihydrate is metabolized primarily by cytochrome P450 (CYP) 3A. The plasma concentration and half-life of Paritaprevir dihydrate can be enhanced by Ritonavir (a CYP450 inhibitor).
1502654-87-6 C53H60F2N8O12 1039.09 Against JFH1/3a-NS5A, DCV was more potent (EC(50) = 0.52 nM) than GS-5885 (EC(50) = 141 nM). DCV sensitivity was increased against JFH1/3a-NS5A-M28V (EC50 = 0.006 nM), A30V (EC(50) = 0.012 nM), and E92A (EC(50) = 0.004 nM) while the NS5A-A30K and -Y93H variants exhibited reduced sensitivity to DCV (EC50 values of 23 nM and 1120 nM, respectively) and to GS-5885 (EC50 values of 1770 nM and 4300 nM, respectively).
GS-5885 was well tolerated and resulted in median maximal reductions in HCV RNA ranging from 2.3 log(10) IU/ml (1 mg QD) to 3.3 log(10) IU/ml (10 mg QD in genotype 1b and 30 mg QD). E(max) modeling indicated GS-5885 30 mg was associated with>95% of maximal antiviral response to HCV genotype 1a. HCV RNA reductions were generally more sustained among patients with genotype 1b vs. 1a. Three of 60 patients had a reduced response and harbored NS5A-resistant virus at baseline. NS5A sequencing identified residues 30 and 31 in genotype 1a, and 93 in genotype 1b as the predominant sites of mutation following GS-5885 dosing. Plasma pharmacokinetics was consistent with QD dosing.
1535212-07-7 C40H52F4N6O9S 868.93 Voxilaprevir (GS-9857) is a noncovalent, reversible inhibitor of HCV NS3/4A protease inhibitor (PI) with pangenotypic antiviral activity. Voxilaprevir inhibits genotype 1b and 3a wild-type NS3 proteases with Ki values of 0.038 nM and 0.066 nM, respectively. Voxilaprevir is an orally active direct-acting antiviral agent (DAA) and can be used for HCV infection research.
1606150-08-6 C40H48D3F4N5O9S 856.94 BMS-986144 targets viral proteases to block replication, providing a research basis for antiviral mechanisms and new drug screening.
1613591-70-0 C25H33F2N6O8P 614.54 This compound is a potent antiviral agent designed to inhibit viral replication by targeting nucleoside analogs. Its mechanism of action makes it a valuable candidate in antiviral research and therapeutic applications.
1620479-63-1 C54H62FN9O8S 1016.19 MK-6169 is a potential antiviral candidate molecule that targets key viral enzymes. It has innovative drug discovery potential and applications in pharmacological and viral inhibition research.
1966138-53-3 C41H52Cl2N8O8 855.81 Coblopasvir-dihydrochloride blocks viral RNA polymerase activity, suppressing replication, widely applied in antiviral mechanism research and candidate drug screening.
20831-76-9 C16H20O9 356.33 Gentiopicroside, a secoiridoid glycoside from Gentiana species, inhibits viral replication. It is widely used in pharmacological mechanism studies, natural product research, and high-value functional ingredient development.
2088243-03-0 C47H48N8O6 820.93 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 C43H56N60O14S 913.1 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.
208940-40-3 C151H185N49O83P14S14 4897 Ac-D-DGla-LI-Cha-C is a synthetic peptide designed to disrupt viral membrane fusion, offering scientific value in antiviral peptide studies and drug innovation.
2172676-02-5 C49H47D7N8O8 890.04 Velpatasvir-[d7] interferes with viral enzyme functions, demonstrating antiviral potential for research and new drug development applications.
2481279-61-0 C25H33F2N6O8P 614.54 AL-611 is an antiviral agent that targets key viral enzymes essential for the replication of RNA viruses. It offers promising therapeutic potential for treating influenza, coronaviruses, and other respiratory viral infections by inhibiting viral replication processes.
2750534-88-2 C40H49BrN6O9S 875.86 Faldaprevir-d6 is deuterium labeled Faldaprevir.
300832-84-2 C40H50N6O8S 774.93 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 C27H45N5O5 519.687 Boceprevir is an HCV protease inhibitor that targets the NS3/4A enzyme. It is commonly used to study hepatitis C viral replication, protease inhibition, and drug resistance mechanisms.
402957-28-2 C36H53N7O6 679.85 Telaprevir is a viral protease inhibitor that suppresses RNA virus replication, offering value in antiviral mechanism and drug development research.
