| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| Other Sizes |
|
Purity: ≥98%
Paritaprevir (formerly ABT-450; ABT450; Veruprevir; Viekirax; Viekira Pak; Technivie) is an acylsulfonamide analog and a component of the anti-HCV drug combination therapies: Viekira Pak (Paritaprevir+ombitasvir, ritonavir and dasabuvir) and Technivie (Paritaprevir+ombitasvir and ritonavir).This non-structural protein 3/4A (NS3/4A) protease inhibitor was authorized in 2015 as a component of combination therapy for the treatment of chronic Hepatitis C. The combination therapy included two versions: Technivie/Viekirax, which included ombitasvir and ritonavir, and Viekira Pak, which included ombitasvir, dasabuvir, and ritonavir. With EC50 values of 1 and 0.21 nM for HCV 1a and 1b, respectively, it inhibits NS3/4A. Abbott Laboratories made the discovery and developed the treatment, which appears to be effective in treating hepatitis C. With an EC50 of 0.09 nM against GT4a, paritaprevir exhibits antiviral activity against HCV GT1-4 and GT6 in vitro (EC50 range: 0.09 to 19 nM). For individuals with hepatitis C virus genotype 1, this combination of ribavirin and ritonavir given for 12 weeks has been estimated to have a 95% rate of sustained virologic response 24 weeks after treatment. Since paritaprevir targets the binding site, treatment resistance is rare. However, mutations at positions 155 and 168 in NS3 have been observed to cause resistance to the medication.
| Targets |
HCV 1a (EC50 = 1 nM); HCV 1b (EC50 = 0.21 nM); SARS-CoV 3CLpro (IC50 = 1.31 μM)
|
||
|---|---|---|---|
| ln Vitro |
Paritaprevir inhibits in vitro the p-glycoprotein (p-gp)[1]. 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, ABT-450 is an effective inhibitor of HCV NS3/4A protease. With a CC50 greater than 37 μM, ABT-450 exhibits an in vitro selectivity index of approximately 37,000 times. ABT-450 has an EC50 of 5.3 nM against the genotype 2a JFH-1 subgenomic replicon, indicating activity against various HCV genotypes[2].
|
||
| ln Vivo |
Paritaprevir achieves maximum concentrations after oral administration in a mean of 4-5 hours, with exposure increases exceeding dose proportionality. Approximately 50% of the total bioavailability occurs when food is administered. It exhibits high plasma protein binding (between 97-99.9%) and 16.7 liters of apparent volume of distribution. Paritaprevir is metabolized primarily by CYP3A4 and CYP3A5[1].
|
||
| Enzyme Assay |
Paritaprevir exhibits antiviral activity in vitro against HCV GT1-4 and GT6 (EC50 range: 0.09 to 19 nM), while its EC50 against GT4a is 0.09 nM.
|
||
| Animal Protocol |
|
||
| References |
| Molecular Formula |
C40H43N7O7S
|
|---|---|
| Molecular Weight |
765.88
|
| Exact Mass |
765.29
|
| Elemental Analysis |
C, 62.73; H, 5.66; N, 12.80; O, 14.62; S, 4.19
|
| CAS # |
1216941-48-8
|
| Related CAS # |
Paritaprevir dihydrate;1456607-71-8
|
| Appearance |
White to off-white powder
|
| SMILES |
CC1=CN=C(C=N1)C(=O)N[C@H]2CCCCC/C=C\[C@@H]3C[C@]3(NC(=O)[C@@H]4C[C@H](CN4C2=O)OC5=NC6=CC=CC=C6C7=CC=CC=C75)C(=O)NS(=O)(=O)C8CC8
|
| InChi Key |
UAUIUKWPKRJZJV-QPLHLKROSA-N
|
| InChi Code |
InChI=1S/C40H43N7O7S/c1-24-21-42-33(22-41-24)35(48)43-32-16-6-4-2-3-5-11-25-20-40(25,39(51)46-55(52,53)27-17-18-27)45-36(49)34-19-26(23-47(34)38(32)50)54-37-30-14-8-7-12-28(30)29-13-9-10-15-31(29)44-37/h5,7-15,21-22,25-27,32,34H,2-4,6,16-20,23H2,1H3,(H,43,48)(H,45,49)(H,46,51)/b11-5-/t25-,26-,32+,34+,40-/m1/s1
|
| Chemical Name |
(1S,4R,6S,7Z,14S,18R)-N-cyclopropylsulfonyl-14-[(5-methylpyrazine-2-carbonyl)amino]-2,15-dioxo-18-phenanthridin-6-yloxy-3,16-diazatricyclo[14.3.0.04,6]nonadec-7-ene-4-carboxamide
|
| Synonyms |
ATB450; ABT 450; ABT-450; Veruprevir; Paritaprevir; Brand name: VIEKIRA PAK
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
|
|||
|---|---|---|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (2.72 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (2.72 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Variability at signature NS5A amino acid positions across HCV GT4 subtypes.Antimicrob Agents Chemother.2015 Nov;59(11):6807-15. |
|---|
Phylogenetic analysis of HCV GT4 baseline sequences.Antimicrob Agents Chemother.2015 Nov;59(11):6807-15. |
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA
