Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Dolutegravir sodium (GSK-1349572A) 是一种高效、口服的 HIV 整合酶链转移抑制剂,在 HIV-1 整合酶催化的链转移中的 IC50值为 2.7 nM, 抑制 HIV-1 病毒在外周血单个核细胞中的复制,IC50为 0.51 nM。它对 Y143R,N155H 和 G140S/Q148H 突变体也保持高效。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 378 | 现货 | ||
2 mg | ¥ 548 | 现货 | ||
5 mg | ¥ 913 | 现货 | ||
10 mg | ¥ 1,330 | 现货 | ||
25 mg | ¥ 2,820 | 现货 | ||
50 mg | ¥ 4,270 | 现货 | ||
100 mg | ¥ 5,970 | 现货 | ||
500 mg | ¥ 12,300 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 975 | 现货 |
产品描述 | Dolutegravir sodium (GSK-1349572A) salt(DTG; GSK1349572) is an HIV integrase inhibitor(IC50: 2.7 nM), modest activity against raltegravir-resistant signature mutants Y143R, Q148K, N155H, and G140S/Q148H. |
靶点活性 | HIV integrase:2.7 nM |
体外活性 | Dolutegravir(S/GSK1349572) inhibits HIV-1 integrase-catalyzed strand transfer with a 50% inhibitory concentration (IC50) of 2.7 nM. S/GSK1349572 inhibits both the HIV integration reaction strand transfer step in vitro and HIV replication in cells with similar potencies. The inhibitor has no effect on total viral DNA synthesis in infected cells but blocks the integration of viral DNA into host DNA with the same potency as its antiviral effect[1]. |
体内活性 | The bioavailability of dolutegravir was high when administered as a solution, but was limited by dissolution rate or solubility when administered as a suspension. Dolutegravir is the major circulating component in mice, rats, and monkeys, with direct ether glucuronidation shown to be the primary biotransformation pathway. Dolutegravir is primarily eliminated via the feces either unabsorbed or by hydrolysis of the glucuronide or glucose conjugate[2]. |
细胞实验 | In vitro growth inhibition (cytotoxicity) studies are conducted with S/GSK1349572 in proliferating human leukemic and lymphomic cell lines (IM-9, U-937, MT-4, and Molt-4) as well as in stimulated and unstimulated human PBMCs. ATP levels are quantified by using the CellTiter-Glo luciferase reagent to measure the ability of a compound to inhibit cell growth as an indicator of the compound's potential for cytotoxicity.(Only for Reference) |
别名 | 度鲁特韦钠, GSK1349572, 度鲁特韦钠盐, GSK-1349572A |
分子量 | 441.36 |
分子式 | C20H18F2N3NaO5 |
CAS No. | 1051375-19-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 4.41 mg/mL (10 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.2657 mL | 11.3286 mL | 22.6572 mL | 56.6431 mL |
5 mM | 0.4531 mL | 2.2657 mL | 4.5314 mL | 11.3286 mL | |
10 mM | 0.2266 mL | 1.1329 mL | 2.2657 mL | 5.6643 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。
Dolutegravir sodium 1051375-19-9 Microbiology/Virology Proteases/Proteasome HIV Protease inhibit S/GSK1349572 GSK 1349572 度鲁特韦钠 GSK-1349572 Human immunodeficiency virus HIV GSK1349572 HIV Integrase 度鲁特韦钠盐 Dolutegravir GSK-1349572A Inhibitor inhibitor