| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
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Tegobuvir (GS-9190; GS-333126) is a novel and potent non-nucleoside polymerase/HCV NS5B polymerase inhibitor with antiviral effects. Tegobuvir (GS-9190) exhibited EC(50)s of <16 nM against genotype 1 and >100 nM for other genotypes tested. Tegobuvir is highly efficient in curing cells from HCV replicon and in delaying/preventing the development of drug resistance. GS-9190 represents a novel class of nonnucleoside polymerase inhibitors that interact with NS5B likely through involvement of the β-hairpin in the thumb subdomain.
| ln Vitro |
In a dose-dependent manner, tigobivir quickly raised the percentage of replicons containing the Y448H mutation. Y448H was expressed by 1.2%, 6.8%, and >50% of the replicon population at 1, 10, and 20 times the 50% effective concentration of tegobuvir, respectively, following three days of therapy [1]. Through a special chemical activation and subsequent direct contact with the NS5B protein, tigobuvir demonstrates anti-HCV efficacy. When tegobuvir is administered to HCV subgenomic replicon cells, NS5B is changed and exhibits markedly altered mobility on SDS-PAGE gels [2]. Tigobuvir exhibits anti-GT1a and anti-GT1b activity, with mean EC50 values of 19.8 and 1.5 nM, correspondingly. The tegobuvir EC50 for the genotype 3a, 4a, and 6a Con chimeras was more than 100 nM. The GT3a, 4a, and 6a chimeric replicons' F445C NS5B mutation brought back tegobuvir potency to EC50 values similar to GT1a [3].
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| References |
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| Additional Infomation |
Tegobuvir has been investigated for the treatment of Hepatitis C, Chronic.
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| Molecular Formula |
C25H14F7N5
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|---|---|
| Molecular Weight |
517.4108
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| Exact Mass |
517.113
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| CAS # |
1000787-75-6
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| PubChem CID |
23649154
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| Appearance |
White to off-white solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
558.0±60.0 °C at 760 mmHg
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| Flash Point |
291.3±32.9 °C
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| Vapour Pressure |
0.0±1.5 mmHg at 25°C
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| Index of Refraction |
1.605
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| LogP |
4.07
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
37
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| Complexity |
765
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
XBEQSQDCBSKCHJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H14F7N5/c26-19-4-2-1-3-17(19)23-33-21-9-10-37(13-22(21)34-23)12-15-6-8-20(36-35-15)16-7-5-14(24(27,28)29)11-18(16)25(30,31)32/h1-11,13H,12H2
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| Chemical Name |
5-[[6-[2,4-bis(trifluoromethyl)phenyl]pyridazin-3-yl]methyl]-2-(2-fluorophenyl)imidazo[4,5-c]pyridine
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| Synonyms |
GS9190 GS-333126 GS 9190 GS333126 GS-9190
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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 : ≥ 50 mg/mL (~96.64 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.75 mg/mL (5.32 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 27.5 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: ≥ 2.75 mg/mL (5.32 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 27.5 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 | 1.9327 mL | 9.6635 mL | 19.3270 mL | |
| 5 mM | 0.3865 mL | 1.9327 mL | 3.8654 mL | |
| 10 mM | 0.1933 mL | 0.9664 mL | 1.9327 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.
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