Paritaprevir (ABT-450)

Paritaprevir (ABT-450) is a nonstructural (NS) protein 3/4A protease inhibitor.

Paritaprevir (ABT-450) Chemical Structure

Paritaprevir (ABT-450) Chemical Structure

CAS: 1216941-48-8

Selleck's Paritaprevir (ABT-450) has been cited by 1 publication

Purity & Quality Control

Batch: S540401 DMSO] 100 mg/mL] false] ] ] false] ] ] false Purity: 99.97%
99.97

Choose Selective HCV Protease Inhibitors

Biological Activity

Description Paritaprevir (ABT-450) is a nonstructural (NS) protein 3/4A protease inhibitor.
Targets
HCV genotype 1b [1]
(in replicon cell culture assays)
HCV genotype 1a [1]
(in replicon cell culture assays)
0.21 nM(EC50) 1 nM(EC50)
In vitro
In vitro Paritaprevir inhibits p-glycoprotein (p-gp) in vitro[1]. 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[2].
In Vivo
In vivo After 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[1].
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

Chemical lnformation & Solubility

Molecular Weight 765.88 Formula

C40H43N7O7S

CAS No. 1216941-48-8 SDF --
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
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (130.56 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

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In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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