产品说明书

Dolutegravir

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Chemical Structure| 1051375-16-6 同义名 : 多替拉韦 ;S/GSK1349572;GSK1349572
CAS号 : 1051375-16-6
货号 : A374780
分子式 : C20H19F2N3O5
纯度 : 98%
分子量 : 419.379
MDL号 : MFCD20488027
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 9 mg/mL(21.46 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：

IP 2% DMSO+2% Tween80+40% PEG300+water 2 mg/mL clear

PO 0.5% CMC-Na 70 mg/mL suspension

生物活性
描述 Dolutegravir is a highly potent and orally bioavailable inhibitor of HIV integrase strand transfer, with an IC50 of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. It effectively inhibits HIV-1 viral replication with an IC50 of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir also maintains significant potency against HIV-1 mutants Y143R, N155H, and G140S/Q148H (EC50=3.6-5.8 nM)[1][2].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
MDCK2 cells Function assay Inhibition of human OCT2 expressed in MDCK2 cells using [14C]metformin as substrate by liquid scintillation counting analysis 23132334
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00867152 Healthy Volunteer Phase 1 Completed - United States, New York ... 展开 >> GSK Investigational Site Buffalo, New York, United States, 14202 收起 <<
NCT00858455 Healthy Volunteer Phase 1 Completed - United States, New York ... 展开 >> GSK Investigational Site Buffalo, New York, United States, 14202 收起 <<
NCT01302847 HIV Infections Phase 1 Phase 2 Recruiting June 30, 2023 -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.38mL

0.48mL

0.24mL

11.92mL

2.38mL

1.19mL

23.84mL

4.77mL

2.38mL
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]Hare S, et al. Structural and functional analyses of the second-generation integrase strand transfer inhibitor dolutegravir (S/GSK1349572). Mol Pharmacol. 2011 Oct;80(4):565-72.

[3]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.