research use only
Cat.No.S5404
| Related Targets | HDAC Caspase Proteasome Secretase MMP Cysteine Protease Tyrosinase DPP HIV Protease Serine Protease |
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| Other HCV Protease Inhibitors | Danoprevir Lomibuvir (VX-222) Asunaprevir Tizoxanide PSI-6206 (GS-331007) 2'-C-Methylcytidine Tegobuvir Herba taxilli Extract Mecarbinate |
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In vitro |
DMSO
: 100 mg/mL
(130.56 mM)
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In vivo |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
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| Molecular Weight | 765.88 | Formula | C40H43N7O7S |
Storage (From the date of receipt) | |
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| CAS No. | 1216941-48-8 | -- | Storage of Stock Solutions |
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| Synonyms | N/A | Smiles | CC1=CN=C(C=N1)C(=O)NC2CCCCCC=CC3CC3(NC(=O)C4CC(CN4C2=O)OC5=NC6=CC=CC=C6C7=CC=CC=C75)C(=O)NS(=O)(=O)C8CC8 | ||
| Targets/IC50/Ki |
HCV genotype 1b
(in replicon cell culture assays) 0.21 nM(EC50)
HCV genotype 1a
(in replicon cell culture assays) 1 nM(EC50)
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| In vitro |
Paritaprevir (ABT-450) inhibits p-glycoprotein (p-gp) in vitro. It 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 this compound is more than 37 μM, resulting in an in vitro selectivity index of ≥37,000-fold. It also demonstrates activity across multiple HCV genotypes, with an EC50 of 5.3 nM against the genotype 2a JFH-1 subgenomic replicon.
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| In vivo |
After oral administration, paritaprevir (ABT-450) 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 an apparent volume of distribution of 16.7 L. Metabolism occurs via CYP3A4 (predominantly) and CYP3A5.
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References |
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(data from https://clinicaltrials.gov, updated on 2024-05-22)
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT02581020 | Completed | Hepatitis C Virus |
AbbVie |
January 14 2016 | -- |
| NCT02534870 | Completed | Healthy Volunteer |
AbbVie |
September 2015 | Phase 1 |
| NCT02734173 | Completed | Hepatitis C |
Ottawa Hospital Research Institute|AbbVie |
July 2015 | Phase 4 |
| NCT01911845 | Completed | Chronic Hepatitis C Infection|Chronic Hepatitis C |
AbbVie |
April 2013 | Phase 2 |
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