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Paritaprevir (ABT-450) HCV Protease inhibitor

Name: Paritaprevir (ABT-450)
Brand: Selleck Chemicals
SKU: S5404
Availability: InStock
Rating: 5 (2 reviews)

Cat.No.S5404

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

Chemical Structure

Molecular Weight: 765.88

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

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

99.97

Related Targets	HDAC Caspase MMP Cysteine Protease DPP Tyrosinase HIV Protease Proteasome Serine Protease Secretase PCSK9 Glutaminase Acyltransferase Thrombin Cathepsin B MALT PAD PREP Neprilysin SGK Aminopeptidase 3C-Like Protease PGDS GOT
Related Products	Lomibuvir (VX-222) Danoprevir Asunaprevir PSI-6206 (GS-331007)

Chemical Information, Storage & Stability

Molecular Weight	765.88	Formula	C₄₀H₄₃N₇O₇S	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1216941-48-8	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
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

Solubility

In vitro
Batch:

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

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5mg/ml (6.53mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.71mg/ml (0.93mM)	Taking the 1 mL working solution as an example, add 50 μL of 14.2 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

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.

Mechanism of Action

Targets/IC₅₀/Ki	HCV genotype 1b ^[1] (in replicon cell culture assays) 0.21 nM(EC50) HCV genotype 1a ^[1] (in replicon cell culture assays) 1 nM(EC50)
In vitro	Paritaprevir (ABT-450) inhibits p-glycoprotein (p-gp) in vitro^[1]. 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^[2].
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^[1].
References	https://pubmed.ncbi.nlm.nih.gov/26059288/ https://pubmed.ncbi.nlm.nih.gov/25451053/

Clinical Trial Information

(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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