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首页-小分子抑制剂&激动剂-Antibiotics and Antivirals-HIV-Dolutegravir
Dolutegravir

Chemical Structure : Dolutegravir

CAS No.: 1051375-16-6

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Dolutegravir (GSK1349572;GSK-1349572;GSK 1349572)

货号: PC-43417Not For Human Use, Lab Use Only.

Dolutegravir (GSK1349572) is a potent, next-generation HIV integrase (IN) inhibitor, inhibits HIV-1 integrase-catalyzed strand transfer with IC50 of 2.7 nM.

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5 mg ￥980 In stock
25 mg ￥2780 In stock
100 mg ￥7480 In stock
500 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Dolutegravir (GSK1349572) is a potent, next-generation HIV integrase (IN) inhibitor, inhibits HIV-1 integrase-catalyzed strand transfer with IC50 of 2.7 nM; inhibits HIV-1 replication in PBMCs, MT-4 cells and in the PHIV assay with EC50 of 0.51, 0.71 and 2.2 nM, respectively; demonstrates activity against site-directed molecular clones containing the raltegravir-resistant signature mutations Y143R, Q148K, N155H, and G140S/Q148H; exhibits excellent anti-HIV activity in combination with representative approved antiretroviral agents in vivo.

HIV Infection

Approved

物理化学性质&存储条件

分子量 419.3788
分子式 C20H19F2N3O5
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

DMSO: 10 mg/mL
Chemical Name/SMILES

2H-Pyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazine-9-carboxamide, N-[(2,4-difluorophenyl)methyl]-3,4,6,8,12,12a-hexahydro-7-hydroxy-4-methyl-6,8-dioxo-, (4R,12aS)-

参考文献

1. Kobayashi M, et al. Antimicrob Agents Chemother. 2011 Feb;55(2):813-21.

2. Garrido C, et al. Antiviral Res. 2011 Jun;90(3):164-7.

3. Hightower KE, et al. Antimicrob Agents Chemother. 2011 Oct;55(10):4552-9.

4. Hare S, et al. Mol Pharmacol. 2011 Oct;80(4):565-72.

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