特拉匹韦 T6190

Product Introduction
Bioactivity


英文名: Telaprevir

描述: Telaprevir (Incivek) 是一种选择性可逆的HCV NS3-4A 蛋白酶抑制剂，作用于基因 1型 (H 株) NS3 蛋白酶结构域和 NS4A 辅因子肽，Ki 为 7 nM。它也是 SARS-CoV-2 3CLpro 抑制剂。

细胞实验: 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)

激酶实验: 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

体外活性: 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赖的裂解（18.7%）和SEAP（18.4%）从肝脏到血液的分泌中.在基因型1b HCV感染人肝细胞的小鼠中,Telaprevir（200 mg/kg）处理1周可使HCV RNA降低,和MK-0608（50 mg/kg）联用处理小鼠,持续4周,可完全除去鼠体内病毒.

体内活性: Telaprevir （17.5 μM）完全消除复制细胞中HCV RNA,停止处理13天后也不再出现。Telaprevir和IFN-α联用可适度提高协同作用,降低HCV RNA复制并抑制耐药突变,但无明显毒性。Telaprevir时间依赖性地促进对HCV RNA复制的抑制,温育24, 48, 72和120小时,则IC50值分别为 0.574 μM, 0.488 μM, 0.210 μM和0.139 μM。在Con1(基因型 1b) 亚基因组HCV复制细胞中,Telaprevir抑制丙型肝炎病毒NS3-4A丝氨酸蛋白酶,导致病毒多聚蛋白加工受抑制,且随后使病毒RNA复制,全部HCV RNA水平和蛋白水平降低,这种作用存在时间和剂量依赖性。Telaprevir处理HCV复制细胞,亲本Huh-7和HepG2细胞48小时后,对细胞没有毒性。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 125 mg/mL (183.9 mM)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
H2O : < 1 mg/mL (insoluble or slightly soluble)


关键字: Inhibitor | Hepatitis C virus | SARS-CoV | LY570310 | VX950 | HCV Protease | SARS coronavirus | MP424 | LY 570310 | VX 950 | HCV | Telaprevir | inhibit | MP 424

相关产品: AG-1478 | FGI-106 tetrahydrochloride | Elbasvir | Sofosbuvir | R-1479 | ACH-806 | Daclatasvir dihydrochloride | Mulberroside C | Chlorcyclizine | Artemisinin

相关库: Drug Repurposing Compound Library | Approved Drug Library | Anti-Cancer Drug Library | Bioactive Compounds Library Max | Anti-Metabolism Disease Compound Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | Anti-Cancer Approved Drug Library | EMA Approved Drug Library | Protease Inhibitor Library

特拉匹韦 T6190信息由TargetMol中国为您提供，如您想了解更多关于特拉匹韦 T6190报价、型号、参数等信息，欢迎来电或留言咨询。

注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途