Paritaprevir (ABT-450) (C09-1017-064)

InformationParitaprevir (ABT-450) Paritaprevir (ABT-450) is a nonstructural (NS) protein 3/4A protease inhibitor.TargetsHCV genotype 1b (in replicon cell culture assays); HCV genotype 1a (in replicon cell culture assays) 0.21 nM(EC50); 1 nM(EC50)In vitroParitaprevir inhibits p-glycoprotein (p-gp) in vitro. ABT-450 is an efficacious inhibitor of HCV NS3/4A protease, with 50% effective concentration values of 1.0, 0.21, 5.3, 19, 0.09, and 0.69 nM against stable HCV replicons with NS3 protease from genotypes 1a, 1b, 2a, 3a, 4a, and 6a, respectively. The CC50 of ABT-450 is more than 37 μM, resulting in an in vitro selectivity index of ≥37,000-fold. ABT-450 demonstrates activity across multiple HCV genotypes, with an EC50 of 5.3 nM against the genotype 2a JFH-1 subgenomic replicon.In vivoAfter oral administration, paritaprevir reaches maximum concentrations in a mean of 4-5 h with increases in exposure more than dose proportional. Absolute bioavailability is about 50% after administering with food. It displays high (about 97-99.9 %) plasma protein binding and has apparent volumes of distribution of 16.7L. Paritaprevir metabolism occurs via CYP3A4 (predominantly) and CYP3A5. Specification: 0.98 Molecular Formula: C40H43N7O7S Molecular Weight: 765.88 PubChem CID: 45110509 Isomeric SMILES: CC1=CN=C(C=N1)C(=O)N[C@H]2CCCCC/C=C/[C@@H]3C[C@]3(NC(=O)[C@@H]4C[C@H](CN4C2=O)OC5=NC6=CC=CC=C6C7=CC=CC=C75)C(=O)NS(=O)(=O)C8CC8 Related Documents: https://ald-pub-files.oss-cn-shanghai.aliyuncs.com/aladdinsci/pdp/sds/1/P413284-SCI_49a32ae5efa5704cfc7d0bd9a5133086.pdf