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Dolutegravir

Chemical Structure Dolutegravir

CAS No.: 1051375-16-6

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Dolutegravir(GSK1349572;GSK-1349572;GSK 1349572)

Catalog No.: GY06092Research Only, Not for Human Use!

Dolutegravir (GSK1349572) is a potent, next-generation HIV integrase (IN) inhibitor, inhibits HIV-1 integrase-catalyzed strand transfer with IC50 of 2

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Purity & Documentation Purity: > 98%(HPLC) Select Batch:

Biological Activity

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.

Physicochemical Properties

M.Wt 419.3788
Formula C20H19F2N3O5
CAS No. 1051375-16-6
Storage
Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 3 Month
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Solubility

10 mM in DMSO
Chemical Name 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)-

Clinical Information

HIV Infection
Approved

References

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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