| Description | 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. |
| In vitro | Dolutegravir(S/GSK1349572)以2.7 nM的50%抑制浓度(IC50)抑制HIV-1整合酶催化的链转移。S/GSK1349572在体外和细胞内抑制HIV整合反应链转移步骤及HIV复制的效能相似。该抑制剂对感染细胞内的总病毒DNA合成无影响，但以与其抗病毒效果相同的效力阻断病毒DNA整合入宿主DNA[1]。 |
| In vivo | 当以溶液形式给予时，dolutegravir的生物可用性较高，但以悬浮液形式给予时，则受到溶解速率或溶解度的限制。在小鼠、大鼠和猴子中，dolutegravir是主要的循环成分，直接的醚类糖醛酸化被证明是主要的生物转化途径。Dolutegravir主要通过粪便排泄，不是未被吸收的形式，就是通过糖醛酸或葡萄糖缀合物的水解[2]。 |
| Cell experiments | 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) |
| Target activity | HIV integrase:2.7 nM |
| Synonyms | 度鲁特韦钠, GSK1349572, 度鲁特韦钠盐, GSK-1349572A |
| molecular weight | 441.36 |
| Molecular formula | C20H18F2N3NaO5 |
| CAS | 1051375-19-9 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 4.41 mg/mL (10 mM) |
| References | 1. Kobayashi M, et al. Antimicrob Agents Chemother. 2011, 55(2):813-21. 2. Moss L, et al. Xenobiotica. 2015, 45(1):60-70. |