Ombitasvir (ABT267; Viekira Pak)

Alias: Viekira Pak (trade name); ABT-267; ABT267; ABT 267
Cat No.:V0073 Purity: ≥98%
Ombitasvir (trade name; Viekira Pak; formerly known as ABT-267) is a novel and potent N-phenylpyrrolidine-based inhibitor of hepatitis C virus (HCV) NS5A with excellent potency, metabolic stability, and pharmacokinetics/PK.
Ombitasvir (ABT267; Viekira Pak) Chemical Structure CAS No.: 1258226-87-7
Product category: HCV Protease
This product is for research use only, not for human use. We do not sell to patients.
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Product Description

Ombitasvir (trade name; Viekira Pak; formerly known as ABT-267) is a novel and potent hepatitis C virus (HCV) NS5A inhibitor based on N-phenylpyrrolidines that exhibits good pharmacokinetics/PK, metabolic stability, and potency. Ombitasvir was discovered to be a pan-genotypic HCV inhibitor, with an EC50 range of 366 pM against GT6a and 1.7-19.3 pM against GT1a, -1b, -2a, -2b, -3a, -4a, and -5a. In treatment-naive HCV GT1-infected subjects, it reduced HCV RNA up to 3.10 log10 IU/mL during a 3-day monotherapy. Under the brand name Viekira Pak, ombitasvir has received FDA approval for use in combination with paritaprevir, ritonavir, and dasabuvir as antiviral medications.

Biological Activity I Assay Protocols (From Reference)
Targets
HCV (IC50 = 0.82 to 19.3 pM); HCV (IC50 = 366 pM)
ln Vitro
Ombitasvir (ABT-267) is a picomolar potency, pan-genotypic activity, and 50% effective concentrations (EC50s) of 0.82 to 19.3 pM against HCV genotypes 1 to 5 and 366 pM against genotype 6a hepatitis C virus (HCV) NS5A inhibitor. When it comes to genotype 1a-H77 and genotype 1b-Con1 subgenomic replicons, ombitasvir's EC50 values are 14.1 and 5.0 pM, respectively[1].
ln Vivo
N/A
Enzyme Assay
The techniques previously described were used to quantify how different amino acid variants affected an inhibitor's activity in HCV replicon cell culture assays. In short, using the Change-IT multiple-mutation site-directed mutagenesis kit (Affymetrix, Santa Clara, CA), the resistance-associated variants in NS5A were each introduced into the genotype 1a-H77 or 1b-Con1 or one of the chimeric genotype 2 to 6 replicons. After sequence analysis verified the variant's existence, the plasmid was linearized and the HCV subgenomic RNA was extracted using the TranscriptAid T7 high-yield transcription kit (Fermentas, Glen Burnie, MD). Through electroporation, a Huh-7 cell line was transfected with the variant-containing replicon RNA in a temporary experiment. As mentioned in the earlier sections, the EC50s were computed.
Cell Assay
A genotype 1b-Con1 HCV replicon-based shuttle vector cassette lacking the Neo gene but containing a luciferase reporter was created to evaluate the NS5A gene phenotypes in patients infected with HCV genotypes 1 through 6. 90 nucleotides upstream of NS5A in the 3′ end of NS4B, a NotI restriction site was cloned into the 1b-Con1 subgenomic replicon vector, and a ClaI site was cloned after the NS5A amino acid 413 codon. The NotI and ClaI restriction sites were crossed with the NS5A region from patients with genotype 1 infection. Ombitasvir's ability to inhibit the NS5A region of non-genotype 1 HCV, which contains amino acids 1 through 214, was assessed using the 1b-Con1 shuttle vector with NotI and BlpI restriction sites (discussed in the preceding section). An amplified copy of the NS5A gene was ligated into the shuttle vector using clinical samples. One transient assay involved electroporating each clinical sample's HCV subgenomic replicon RNA containing the NS5A gene into a cell line derived from Huh-7. Ombitasvir was present during the four days that the cells were cultured. Following the procedure previously mentioned, the luciferase activity in the cells was determined.
Animal Protocol
N/A
N/A
References

[1]. Antimicrob Agents Chemother . 2015 Feb;59(2):979-87.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C50H67N7O8
Molecular Weight
894.11
Exact Mass
893.51
Elemental Analysis
C, 67.17; H, 7.55; N, 10.97; O, 14.32
CAS #
1258226-87-7
Appearance
Solid powder
SMILES
CC(C)[C@@H](C(=O)N1CCC[C@H]1C(=O)NC2=CC=C(C=C2)[C@@H]3CC[C@H](N3C4=CC=C(C=C4)C(C)(C)C)C5=CC=C(C=C5)NC(=O)[C@@H]6CCCN6C(=O)[C@H](C(C)C)NC(=O)OC)NC(=O)OC
InChi Key
PIDFDZJZLOTZTM-KHVQSSSXSA-N
InChi Code
InChI=1S/C50H67N7O8/c1-30(2)42(53-48(62)64-8)46(60)55-28-10-12-40(55)44(58)51-35-20-14-32(15-21-35)38-26-27-39(57(38)37-24-18-34(19-25-37)50(5,6)7)33-16-22-36(23-17-33)52-45(59)41-13-11-29-56(41)47(61)43(31(3)4)54-49(63)65-9/h14-25,30-31,38-43H,10-13,26-29H2,1-9H3,(H,51,58)(H,52,59)(H,53,62)(H,54,63)/t38-,39-,40-,41-,42-,43-/m0/s1
Chemical Name
methyl N-[(2S)-1-[(2S)-2-[[4-[(2S,5S)-1-(4-tert-butylphenyl)-5-[4-[[(2S)-1-[(2S)-2-(methoxycarbonylamino)-3-methylbutanoyl]pyrrolidine-2-carbonyl]amino]phenyl]pyrrolidin-2-yl]phenyl]carbamoyl]pyrrolidin-1-yl]-3-methyl-1-oxobutan-2-yl]carbamate
Synonyms
Viekira Pak (trade name); ABT-267; ABT267; ABT 267
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 Data
Solubility (In Vitro)
DMSO: >100 mg/mL
Water: N/A
Ethanol: N/A
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 1.1184 mL 5.5922 mL 11.1843 mL
5 mM 0.2237 mL 1.1184 mL 2.2369 mL
10 mM 0.1118 mL 0.5592 mL 1.1184 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.

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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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.
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Clinical Trial Information
NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02487199 Completed Drug: ombitasvir/paritaprevir
/ritonavir and dasabuvir
Drug: ombitasvir/paritaprevir
/ritonavir
Hepatitis C Virus
(HCV)
AbbVie September 30, 2015 Phase 3
NCT02476617 Completed Drug: dasabuvir
Drug: ribavirin
Chronic Hepatitis C
Hepatitis C (HCV)
AbbVie June 2015 Phase 3
NCT02399345 Completed Drug: sofosbuvir (SOF)
Drug: ribavirin (RBV)
Chronic Hepatitis C Virus
(HCV Infection Genotype 1)
AbbVie March 2015 Phase 3
NCT02493855 Completed Drug: Dasabuvir
Drug: Ribavirin (RBV)
Hepatitis C (HCV)
Chronic Hepatitis C
AbbVie June 2015 Phase 2
NCT02581189 Completed Drug: Dasabuvir
Drug: Ribavirin
Chronic Hepatitis C AbbVie October 13, 2015
Biological Data
  • Ombitasvir (ABT-267)

    Alignment of amino acids 1 to 100 of NS5A in the replicon cell lines. Amino acid changes relative to the 1b-Con1 sequence are indicated. Amino acids within each genotype where variants resistant to ombitasvir were selected are highlighted in gray.2015 Feb;59(2):979-87.

  • Ombitasvir (ABT-267)

    HCV RNA viral load during 3-day monotherapy with ombitasvir in HCV genotype 1-infected treatment-naive patients.2015 Feb;59(2):979-87.


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