比克替拉韦
货号:
IB2610
品牌:
Jinpan
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产品简介
有效期 | 2年 |
别名 | 毕卡特韦;GS-9883 |
英文名称 | Bictegravir |
CAS | 1611493-60-7 |
分子式 | C21H18F3N3O5 |
分子量 | 449.38 |
储存条件 | -20℃ |
纯度 | ≥98% |
外观(性状) | Powder |
单位 | 瓶 |
生物活性 | Bictegravir (GS-9883)是一种新型的、有效的HIV-1 integrase抑制剂。[1] |
In Vitro | Bictegravir exhibits potent and selective in vitro antiretroviral activity in both T-cell lines and primary human T lymphocytes, with 50% effective concentrations ranging from 1.5 to 2.4 nM and selectivity indices up to 8,700 relative to cytotoxicity. Bictegravir inhibits the strand transfer activity with an IC50 of 7.5 ± 0.3 nM. Relative to its inhibition of strand transfer activity, Bictegravir is a much weaker inhibitor of 3′-processing activity of HIV-1 integrase, with an IC50 of 241 ± 51 nM. Bictegravir potently inhibits HIV-1 replication in both MT-2 and MT-4 cells with EC50s of 1.5 and 2.4 nM, respectively, and selectivity indices (50% cytotoxic concentration [CC50]/EC50) of ~6,800 in MT-2 cells and ~1,500 in MT-4 cells[1]. |
SMILES | O=C1N([C@](CC2)([H])C[C@]2([H])O3)[C@@]3([H])CN(C=C(C(NCC(C(F)=CC(F)=C4)=C4F)=O)C5=O)C1=C5O |
靶点 | HIV-1 integrase |
数据来源文献 | [1] Tsiang M, et al. Antimicrob Agents Chemother. 2016, 60(12):7 |
规格 | 5mg 10mg |
是一种新型的、有效的HIV-1 integrase抑制剂。