| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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Purity: ≥98%
Dasabuvir (formerly known as ABT-333; ABT333; trade name Exviera, Viekira Pak, Viekira XR) is a nonnucleoside inhibitor of the RNA-dependent RNA polymerase encoded by the hepatitis C virus (HCV) NS5B gene. It inhibited recombinant NS5B polymerases derived from HCV genotype 1a and 1b clinical isolates, with IC50 values between 2.2 and 10.7 nM, and was at least 7,000-fold selective for the inhibition of HCV genotype 1 polymerases over human/mammalian polymerases. Dasabuvir is an FDA approved antiviral medication for the treatment of hepatitis C. It is often used together with the combination medication ombitasvir/paritaprevir/ritonavir specifically for hepatitis C virus (HCV) type 1.
| Targets |
HCV genotype 1b N(IC50=2.2 ± 0.3 nM);HCV genotype 1a H77(IC50=2.8 ± 0.2 nM);HCV genotype 1b BK(IC50=3.1 ± 0.21 nM);HCV genotype 1b Con1(IC50=0.7 ± 1.4 nM)
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| ln Vitro |
Dasabuvir is at least 7,000-fold selective for the inhibition of HCV genotype 1 polymerases over human/mammalian polymerases. Dasabuvir inhibits the polymerase enzymatic activity of genotype 1 laboratory strain enzymes (H77, BK, N, and Con1 strains), as well as enzymes produced from polymerase genes from HCV genotype 1-infected subjects, with IC50s between 2.2 and 10.7 nM. Dasabuvir inhibits replication of HCV subgenomic replicons in cell culture assays, with EC50 values of 7.7 and 1.8 nM against genotype 1a (H77) and 1b (Con1), respectively. In the presence of 40% human plasma, there is a 12- to 13-fold decrease in inhibitory potency, yielding EC50s of 99 and 21 nM for HCV genotype 1a (H77) and 1b (Con1) replicons, respectively.
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| ln Vivo |
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| Enzyme Assay |
the inhibition of human and mammalian DNA polymerases was evaluated by Replizyme Ltd. (Heslington, United Kingdom). The DNA-dependent RNA polymerase activity for human RNA polymerases II and III was measured using polymerases present in a HeLa cell extract and DNA templates containing promoters specific for either polymerase II or polymerase III. α-Amanitin, a potent inhibitor of human polymerase II and a modest inhibitor of polymerase III, was used as a control. The reaction mixtures contained 20 mM Tris-HCl (pH 8.0), 20% glycerol, 100 mM KCl, 1 mM dithiothreitol (DTT), 0.2 mM EDTA, 6 mM MgCl2, and either 1 μg/μl pAdVAntage plasmid (Promega, Madison, WI) (for the polymerase III assay) or 25 ng/μl cytomegalovirus (CMV) promoter DNA (Promega, Madison, WI) (for the polymerase II assay). The reaction mixtures also contained HeLa cell nuclear extract (ProteinOne, Rockville, MD), 400 μM ATP, CTP, and UTP, and 16 μM GTP and [α-33P]GTP. The reaction mixtures were incubated for 1 h at 30°C, quenched with the addition of proteinase K, SDS, and EDTA, incubated for 30 min at 56°C, and then analyzed on a Criterion Bio-Rad 5% acrylamide Tris-borate-EDTA (TBE)-urea gel. The gel was dried and placed on a PhosphorImager screen for overnight exposure. The volumes of the product bands were measured, and the percent inhibition was calculated; IC50 values were calculated using the following equation: % inhibition = 100[I]/([I] + IC50).
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| Cell Assay |
Dasabuvir (ABT-333) is at least 7,000-fold selective for the inhibition of HCV genotype 1 polymerases over human/mammalian polymerases. Dasabuvir (ABT-333) inhibits the polymerase enzymatic activity of genotype 1 laboratory strain enzymes (H77, BK, N, and Con1 strains), as well as enzymes produced from polymerase genes from HCV genotype 1-infected subjects, with IC50s between 2.2 and 10.7 nM. Dasabuvir (ABT-333) inhibits replication of HCV subgenomic replicons in cell culture assays, with EC50 values of 7.7 and 1.8 nM against genotype 1a (H77) and 1b (Con1), respectively. In the presence of 40% human plasma, there is a 12- to 13-fold decrease in inhibitory potency, yielding EC50s of 99 and 21 nM for HCV genotype 1a (H77) and 1b (Con1) replicons, respectively.
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| Animal Protocol |
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| References |
| Molecular Formula |
C26H27N3O5S
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| Molecular Weight |
493.57
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| Exact Mass |
493.17
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| Elemental Analysis |
C, 63.27; H, 5.51; N, 8.51; O, 16.21; S, 6.50
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| CAS # |
1132935-63-7
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| Related CAS # |
Dasabuvir sodium;1132940-11-4
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| Appearance |
White to off-white solid powder.
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| SMILES |
CS(=O)(NC1=CC=C2C=C(C3=CC(N(C(N4)=O)C=CC4=O)=CC(C(C)(C)C)=C3OC)C=CC2=C1)=O
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| InChi Key |
NBRBXGKOEOGLOI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C26H27N3O5S/c1-26(2,3)22-15-20(29-11-10-23(30)27-25(29)31)14-21(24(22)34-4)18-7-6-17-13-19(28-35(5,32)33)9-8-16(17)12-18/h6-15,28H,1-5H3,(H,27,30,31)
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| Chemical Name |
N-(6-(3-(tert-butyl)-5-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-2-methoxyphenyl)naphthalen-2-yl)methanesulfonamide
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| Synonyms |
ABT333; ABT-333; ABT 333, Dasabuvir; Trade names: Viekira Pak
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO : 46~98 mg/mL ( 93.20 ~198.55 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.07 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 25.0 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: ≥ 2.5 mg/mL (5.07 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.07 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 10% DMSO+40% PEG300+5% Tween-80+45% Saline: ≥ 2.5 mg/mL (5.07 mM) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0261 mL | 10.1303 mL | 20.2606 mL | |
| 5 mM | 0.4052 mL | 2.0261 mL | 4.0521 mL | |
| 10 mM | 0.2026 mL | 1.0130 mL | 2.0261 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.
PBPK simulations of the pharmacokinetic profiles ofdasabuvirfollowing a single intravenous dose (a,b) or oral dose (c,d) in healthy volunteers.Clin Pharmacol Ther. 2017 Oct; 102(4): 679–687. |
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