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描述 | HIV-1 integrase, a member of a polynucleotidyl transferases superfamily, catalyzes the insertion of the viral DNA into the genome of host cells[2]. HIV-1 IN acts as a key component of the Retroviral Pre-Integration Complex (PIC)[3].the HIV-1 replication depends not only on distinct steps but also lens epithelium-derived growth factor/p75 (LEDGF/p75)[4]. HIV-1 integrase (IN) inhibitors are primary drugs in Highly active antiretroviral therapy (HAART) regimens targeting integration step in the HIV-1 life cycle[5]. Lavendustin B is an inhibitor of HIV-1 integrase interaction with LEDGF/p75 with an IC50 of 94.07 μM. Lavendustin B is an ATP-competitive GLUT1 inhibitor with a Ki of 15 µM. Lavendustin B is also a weak inhibitor of tyrosine kinases[6]. In HL-60 cells, Lavendustin B (0-1000 µM) inhibits the uptake of methylglucose, deoxyglucose, and dehydroascorbic acid in human erythrocytes in a dose-dependent manner, with 50% inhibition observed at approximately 10-30 µM. Moreover, increasing concentrations of Lavendustin B inhibited, in a dose-dependent manner, the binding of cytochalasin B to human erythrocyte membranes[7]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.74mL 0.55mL 0.27mL |
13.68mL 2.74mL 1.37mL |
27.37mL 5.47mL 2.74mL |
CAS号 | 125697-91-8 |
分子式 | C21H19NO5 |
分子量 | 365.379 |
别名 | |
运输 | 蓝冰 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Inert atmosphere,Store in freezer, under -20°C |
溶解方案 |
DMSO: 50 mg/mL(136.84 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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动物实验配方 |