Tegobuvir GS 333126; GS-9190,98.02%
产品编号:Bellancom-10544| CAS NO:1000787-75-6| 分子式:C25H14F7N5| 分子量:517.40
Tegobuvir 是一种特异性的,共价的 HCV NS5B polymerase 抑制剂。
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Tegobuvir GS 333126; GS-9190
产品介绍 | Tegobuvir 是一种特异性的,共价的 HCV NS5B polymerase 抑制剂。 | ||||||||||||||||
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生物活性 | Tegobuvir is a specific, covalent inhibitor of the HCV NS5B polymerase. | ||||||||||||||||
体外研究 |
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. 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. 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. 西域 has not independently confirmed the accuracy of these methods. They are for reference only. | ||||||||||||||||
体内研究 | |||||||||||||||||
体内研究 | |||||||||||||||||
性状 | Solid | ||||||||||||||||
溶解性数据 |
In Vitro:
DMSO : ≥ 50 mg/mL (96.64 mM) * "≥" means soluble, but saturation unknown. 配制储备液
*
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百
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运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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参考文献 |
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