1. Anti-infection
  2. HCV
  3. Tegobuvir

Tegobuvir (Synonyms: GS 333126; GS-9190)

Cat. No.: HY-10544 Purity: 98.52%
Handling Instructions

Tegobuvir is a specific, covalent inhibitor of the HCV NS5B polymerase.

For research use only. We do not sell to patients.

Tegobuvir Chemical Structure

Tegobuvir Chemical Structure

CAS No. : 1000787-75-6

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 341 In-stock
Estimated Time of Arrival: December 31
5 mg USD 300 In-stock
Estimated Time of Arrival: December 31
10 mg USD 600 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1800 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Based on 4 publication(s) in Google Scholar

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Description

Tegobuvir is a specific, covalent inhibitor of the HCV NS5B polymerase.

In Vitro

Tegobuvir rapidly increases the proportion of replicons with the Y448H mutation in a dose-dependent manner. After 3 days of treatment, 1.2%, 6.8%, and > 50% of the replicon population expresses Y448H with the use of Tegobuvir at 1, 10, and 20 times its 50% effective concentration, respectively[1]. Tegobuvir exerts anti-HCV activity utilizing a unique chemical activation and subsequent direct interaction with the NS5B protein. Treatment of HCV subgenomic replicon cells with Tegobuvir results in a modified form of NS5B with a distinctly altered mobility on a SDS-PAGE gel[2]. Tegobuvir is potent in GT1a and 1b with mean EC50s of 19.8 and 1.5 nM respectively. For genotype 3a, 4a, and 6a Con chimeras, tegobuvir EC50s are all greater than 100 nM. The F445C NS5B mutations in GT3a, 4a, and 6a chimeric replicons restore tegobuvir potency to EC50 levels comparable to GT1a[3].

Clinical Trial
Molecular Weight

517.40

Formula

C₂₅H₁₄F₇N₅

CAS No.

1000787-75-6

SMILES

FC1=CC=CC=C1C2=NC3=CN(CC4=NN=C(C5=CC=C(C(F)(F)F)C=C5C(F)(F)F)C=C4)C=CC3=N2

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 50 mg/mL (96.64 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9327 mL 9.6637 mL 19.3274 mL
5 mM 0.3865 mL 1.9327 mL 3.8655 mL
10 mM 0.1933 mL 0.9664 mL 1.9327 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.75 mg/mL (5.32 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.75 mg/mL (5.32 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[2]

Replicon-containing cells are trypsinized and seeded in cell culture media without G418 in white 96-well plates for EC50 analysis. Stable replicon carrying cell lines are seeded at a density of 5,000 cells per well. Serial threefold dilutions (10 concentrations) of compounds are performed in DMSO followed by further dilution in cell culture media and subsequent addition to cell plates. Compound-treated cells are incubated 72 hours at 37°C in a 5% CO2 incubator. 

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Tegobuvir
Cat. No.:
HY-10544
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