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Dolutegravir sodium

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Chemical Structure| 1051375-19-9 同义名 : 度鲁特韦钠 ;S/GSK1349572 sodium;GSK-1349572A
CAS号 : 1051375-19-9
货号 : A102661
分子式 : C20H18F2N3NaO5
纯度 : 99%
分子量 : 441.361
MDL号 : MFCD28405599
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 2 mg/mL(4.53 mM)，配合低频超声，并水浴加热至45℃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
动物实验配方：

PO 0.5% CMC-Na 50 mg/mL suspension

生物活性
描述 Dolutegravir sodium (S/GSK1349572 sodium) is a potent, orally available inhibitor of HIV integrase strand transfer, exhibiting an IC50 of 2.7 nM against HIV-1 integrase-mediated strand transfer. It effectively suppresses HIV-1 viral replication with an IC50 of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir sodium also maintains high efficacy against HIV-1 mutants Y143R, N155H, and G140S/Q148H, with EC50 values ranging from 3.6 to 5.8 nM[1][2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.27mL

0.45mL

0.23mL

11.33mL

2.27mL

1.13mL

22.66mL

4.53mL

2.27mL
参考文献

[1]Kobayashi M, et al. In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor. Antimicrob Agents Chemother. 2011 Feb;55(2):813-21.

[2]Moss L, et al. The comparative disposition and metabolism of dolutegravir, a potent HIV-1 integrase inhibitor, in mice, rats, and monkeys. Xenobiotica. 2015 Jan;45(1):60-70.