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- Dolutegravir sodium(GSK1349572) 1051375-19-9

- Dolutegravir sodium(GSK1349572) 1051375-19-9
Dolutegravir sodium(GSK1349572) 1051375-19-9
产品描述 描述 Dolutegravir sodium salt(DTG; GSK1349572) is a HIV integrase inhibitor(IC50= 2.7 nM), modest activity against raltegravir-resistant signature mutants Y143R, Q148K, N155H, and G140S/Q148H.
纯度 98%储存/保存方法 Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.基本信息 可溶性/溶解性 200 mM in DMSO生物活性 靶点 HIV integraseIn vitro(体外研究) 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.In vivo(体内研究) 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.参考文献 参考文献 1. Kobayashi M, et al. Antimicrob Agents Chemother. 2011, 55(2), 813-821.
2. Charpentier C, et al. AIDS. 2010 Nov 13;24(17):2753-5.
研究领域 研究领域 Drug DiscoverySmall Molecule DrugLead Compound DiscoveryDolutegravir sodium(GSK1349572) 1051375-19-9温馨提示:本产品仅作科研实验使用,不支持临床等研究
