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Dolutegravir sodium(GSK1349572) 1051375-19-9

简要描述:Dolutegravir sodium(GSK1349572) 1051375-19-9
Dolutegravir sodium salt(DTG; GSK1349572) is a HIV integrase inhibitor(IC50= 2.7 nM),

  • 产品型号:abs47027998
  • 厂商性质:生产厂家
  • 更新时间:2026-01-12
  • 访  问  量:751

详细介绍

品牌absinCAS1051375-19-9
分子式C20H18F2N3NaO5纯度98%
分子量441.36货号abs47027998
规格2mg供货周期现货
主要用途is a HIV integrase inhibitor应用领域化工,生物产业,农林牧渔,制药/生物制药,综合

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 integrase
In 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 Discovery
Dolutegravir 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

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