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Paritaprevir

Cat. No. M8880
Paritaprevir Structure
Synonym:

ABT-450

Size Price Availability
10mg USD 250 4-7 Days
50mg USD 700 4-7 Days
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

Paritaprevir (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 and EC50s of 19, 0.09, and 0.69 nM against replicons containing NS3 protease from genotypes 3a, 4a, and 6a, respectively.

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 765.88
Formula C40H43N7O7S
CAS Number 1216941-48-8
Purity >98%
Solubility DMSO: ≥ 90 mg/mL
Storage at -20°C
References

Ombitasvir/Paritaprevir/Ritonavir Plus Dasabuvir: A Review in Chronic HCV Genotype 1 Infection.
Deeks ED. Drugs. 2015 Jun;75(9):1027-38. PMID: 26059288.

In vitro and in vivo antiviral activity and resistance profile of the hepatitis C virus NS3/4A protease inhibitor ABT-450.
Pilot-Matias T, et al. Antimicrob Agents Chemother. 2015 Feb;59(2):988-97. PMID: 25451053.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Paritaprevir, ABT-450 supplier, HCV Protease, inhibitors

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