[CAS NO. 1216941-48-8] Paritaprevir (ABT-450)

Name: Paritaprevir (ABT-450)
Brand: Arctom Scientific
SKU: SLK-S5404

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PRODUCTS SPECIFICATIONS [1216941-48-8]

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Catalog

SLK-S5404

Brand

Selleck

CAS

1216941-48-8

DESCRIPTION [1216941-48-8]

Overview

MDL	MFCD28411394
Molecular Weight	765.88
Molecular Formula	C40H43N7O7S
SMILES	C(NS(=O)(=O)C1CC1)(=O)[C@]23[C@@](C2)(/C=C\CCCCC[C@H](NC(=O)C=4C=NC(C)=CN4)C(=O)N5[C@](C(=O)N3)(C[C@@H](OC6=C7C(=C8C(=N6)C=CC=C8)C=CC=C7)C5)[H])[H]

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	1.3057 mL	6.5284 mL	13.0569 mL
5 mM	0.2611 mL	1.3057 mL	2.6114 mL
10 mM	0.1306 mL	0.6528 mL	1.3057 mL
50 mM	0.0261 mL	0.1306 mL	0.2611 mL

Description

Paritaprevir (ABT-450) is a nonstructural (NS) 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

Paritaprevir 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 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.

References

[1] Deeks ED. Drugs. 2015, 75(9):1027-38.
[2] Pilot-Matias T, et al. Antimicrob Agents Chemother. 2015, 59(2):988-97.

Synonyms

Cyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxamide, N-(cyclopropylsulfonyl)-1,2,3,6,7,8,9,10,11,13a,14,15,16,16a-tetradecahydro-6-[[(5-methyl-2-pyrazinyl)carbonyl]amino]-5,16-dioxo-2-(6-phenanthridinyloxy)-, (2R,6S,12Z,13aS,14aR,16aS)-

(2R,6S,12Z,13aS,14aR,16aS)-N-(Cyclopropylsulfonyl)-1,2,3,6,7,8,9,10,11,13a,14,15,16,16a-tetradecahydro-6-[[(5-methyl-2-pyrazinyl)carbonyl]amino]-5,16-dioxo-2-(6-phenanthridinyloxy)cyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxamide

Paritaprevir

ABT 450