13585831301
021-59541103 021-60443211
3004967995
13585831301021-59541103 021-604432113004967995
聯系人:高小姐
電話:021-59541103 021-60443211
手機:13585831301
Q Q： 3004967995
Email:3004967995@qq.com
詳細地址：上海嘉定區嘉羅公路1661
化學性質：
| 規格 | 10mM (in 1mL DMSO) 5mg 10mg 50mg |
| CAS | 1000787-75-6 |
| 別名 | GS-333126;GS-9190;GS333126;GS9190 |
| 化學名 | 5-[[6-[2,4-bis(trifluoromethyl)phenyl]pyridazin-3-yl]methyl]-2-(2-fluorophenyl)imidazo[4,5-c]pyridine |
| 分子式 | C25H14F7N5 |
| 分子量 | 517.4 |
| 溶解度 | ≥ 24.95 mg/mL in DMSO, ≥ 100 mg/mL in EtOH |
| 儲存條件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice |
產品描述：
Tegobuvir (TGV) is a non-nucleoside of HCV RNA replication EC50s of ＜ 16 nM against genotype 1 and ＞100 nM for other genotypes. [1, 2]
Tegobuvir inhibited HCV replication by targeting the NS5B polymerase. The NS5B polymerase is an RNA polymerase which is responsible for HCV replication and is RNA-dependent RNA polymerase.[3, 4] The HCV NS5B contains canonical thumb, finger, and palm subdomains.[3]
Tegobuvir has potent activity against genotypes 1a and 1b HCV in HCV replicons in vitro, and in HCV genotype 1-infected patients and GT 1a EC50 is 17-fold higher than that observed in GT 1b.[5] However, It exhibited reduced activity against GT2a replicons and GT2a infectious virus. Furthermore, the C445F mutation selected by tegobuvir caused a 7.1 fold increase in EC50.[2] Thus, it indicated that the mechanism of tegobuvir is related to HCV NS5B. The data from different mutation of NS5B including C316Y, C445F, and Y452H indicated that the inhibitory effect is due to the interaction with the hairpin in the thumb subdomain.[2] But, The mechanism of TGV still has not been clearly defined. TGV does not have any inhibition effect on NS5B enzymatic activity with recombinant NS5B proteins.[5] A decrease in antiviral potency of TGV was observed when a CYP1A inhibitor was combined used in antiviral assays. It demonstrated that TGV binds to the NS5B polymerase after undergoing a multistep metabolic activation pathway.[5] The activity of TGV also is related to the specific glutathione adducts.[5] Besides the sub-type differences, TGV also is less potent against the GT 1b replicon in the HeLa cell line with EC50＞10 M.
When individual patients treated only with tegobuvir with 8 days, it demonstrated median reductions of 1.5 log10 IU/mL in HCV RNA. But, rates of RVR (HCV RNA< 25 IU/mL at week 4) was enhanced when treated with Peg-IFN and RBV at the same time.[5]
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原創作者：上海莼試生物技術有限公司
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普票匯款信息
賬 戶 名：上海生物
開 戶 行：中國銀行山東省分行營業部
賬 號：2169 2341 6278
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