Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Bictegravir (GS-9883) 是一种 HIV-1 整合酶抑制剂,其IC50值为 7.5 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 282 | 现货 | ||
5 mg | ¥ 638 | 现货 | ||
10 mg | ¥ 1,090 | 现货 | ||
25 mg | ¥ 2,130 | 现货 | ||
50 mg | ¥ 3,830 | 现货 | ||
100 mg | ¥ 5,570 | 现货 | ||
500 mg | ¥ 11,500 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 688 | 现货 |
产品描述 | Bictegravir (GS-9883) is a potent inhibitor of HIV-1 integrase (IC50: 7.5 nM). |
靶点活性 | HIV-1 integrase:7.5 nM |
体外活性 | Bictegravir potently inhibits HIV-1 replication in both MT-2 and MT-4 cells with EC50s of 1.5 and 2.4 nM, respectively. Bictegravir inhibits the strand transfer activity with an IC50 of 7.5 nM. Relative to its inhibition of strand transfer activity, Bictegravir is a much weaker inhibitor of the 3′-processing activity of HIV-1 IN, with an IC50 of 241 nM. Bictegravir enhances the accumulation of 2-LTR circles ~5-fold relative to the mock-treated control and reduces the number of authentic integration products in infected cells by 100-fold. Bictegravir exhibits potent antiviral effects in both primary CD4+ T lymphocytes and monocyte-derived macrophages, with EC50s of 1.5 nM and 6.6 nM, respectively, which are comparable to values obtained in T-cell lines[1]. |
细胞实验 | MT-2 cells are infected in bulk culture with HIV-1 IIIb at a cell density of 2×10^6 cells/mL for 3 h at 37°C. Infected MT-2 cells receive either DMSO (mock-treated control) or Bictegravir at a final concentration greater than or equal to 20 times their respective antiviral EC50. These plates are incubated at 37°C for either 12 h (for late reverse transcription product quantification) or 24 h (for 2-LTR circle and Alu-LTR product quantification), after which time the cells are harvested for total DNA isolation. DNA is extracted from each well using the DNA minikit and collected as a 100-μL eluate. TaqMan real-time PCR-quantified 2-LTR junctions, late reverse transcription products, and integration junctions (Alu-LTR) are normalized to the level of host globin gene in each sample[1]. |
别名 | GS-9883 |
分子量 | 449.38 |
分子式 | C21H18F3N3O5 |
CAS No. | 1611493-60-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 80 mg/mL
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Bictegravir 1611493-60-7 Microbiology/Virology Proteases/Proteasome HIV Protease HIV Integrase Inhibitor GS9883 HIV Human immunodeficiency virus inhibit GS-9883 GS 9883 inhibitor