| 名稱 | Telaprevir |
| 描述 | Telaprevir (Incivek) (VX-950) is an effective inhibitor of HCV NS3-4A serine protease (IC50: 0.35 μM). |
| 細胞實驗 | Cells are incubated with various concentrations of Telaprevir for 48 hours. Cell viability is determined by using a tetrazolium (MTS)-based cell viability assay.(Only for Reference) |
| 激酶實驗 | Determination of anti-HCV activity: Stable Huh-7 cells containing the self-replicating, subgenomic HCV replicon, which is identical in sequence to the I377neo/NS3-3'/wt replicon are used for anti-HCV assays. Replicon cells are incubated at 37 °C for the indicated period of time with Telaprevir serially diluted in DMEM plus 2% FBS and 0.5% dimethyl sulfoxide (DMSO). Total cellular RNA is extracted using an RNeasy-96 kit, and the copy number of HCV RNA is determined using a quantitative RTPCR (QRT-PCR) assay for the assessment of 50% inhibitory concentration (IC50 |
| 體外活性 | 在小鼠模型中, Telaprevir（10和25 mg/kg,p.o.） 降低丙型肝炎病毒蛋白酶依賴的裂解（18.7%）和SEAP（18.4%）從肝臟到血液的分泌中.在基因型1b HCV感染人肝細胞的小鼠中,Telaprevir（200 mg/kg）處理1周可使HCV RNA降低,和MK-0608（50 mg/kg）聯(lián)用處理小鼠,持續(xù)4周,可完全除去鼠體內(nèi)病毒. |
| 體內(nèi)活性 | Telaprevir （17.5 μM）完全消除復(fù)制細胞中HCV RNA,停止處理13天后也不再出現(xiàn)。Telaprevir和IFN-α聯(lián)用可適度提高協(xié)同作用,降低HCV RNA復(fù)制并抑制耐藥突變,但無明顯毒性。Telaprevir時間依賴性地促進對HCV RNA復(fù)制的抑制,溫育24, 48, 72和120小時,則IC50值分別為 0.574 μM, 0.488 μM, 0.210 μM和0.139 μM。在Con1(基因型 1b) 亞基因組HCV復(fù)制細胞中,Telaprevir抑制丙型肝炎病毒NS3-4A絲氨酸蛋白酶,導(dǎo)致病毒多聚蛋白加工受抑制,且隨后使病毒RNA復(fù)制,全部HCV RNA水平和蛋白水平降低,這種作用存在時間和劑量依賴性。Telaprevir處理HCV復(fù)制細胞,親本Huh-7和HepG2細胞48小時后,對細胞沒有毒性。 |
| 存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice./Shipping at ambient temperature. |
| 溶解度 | DMSO : 125 mg/mL (183.86 mM), Sonication is recommended.
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
H2O : < 1 mg/mL (insoluble or slightly soluble)
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| 關(guān)鍵字 | VX950 | VX 950 | Telaprevir | SARS-CoV | SARSCoV | SARS coronavirus | MP424 | MP 424 | LY570310 | LY 570310 | Inhibitor | inhibit | Hepatitis C virus | HCVProtease | HCV Protease | HCV NS3-4A serine protease | HCV |
| 相關(guān)產(chǎn)品 | Umifenovir hydrochloride | Chloroquine phosphate | Dexamethasone | Hydroxychloroquine | Artemisinin | EIDD-1931 | Methyl 2-amino-5-bromobenzoate | Silymarin | Nirmatrelvir | Ribavirin | Molnupiravir | Remdesivir |
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