Dolutegravir
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Dolutegravir
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CAS No:
1051375-16-6
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Formula:
C20H19F2N3O5
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Chemical Name:
Dolutegravir
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Synonyms:
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)-;(4R,12aS)-N-[(2,4-Difluorophenyl)methyl]-3,4,6,8,12,12a-hexahydro-7-hydroxy-4-methyl-6,8-dioxo-2H-pyrido[1′,2′:4,5]pyrazino[2,1-b][1,3]oxazine-9-carboxamide;GSK 1349572;S/GSK1349572;Dolutegravir;Tivicay;Soltegravir;(4R,9aS)-5-Hydroxy-4-methyl-6,10-dioxo-3,4,6,9,9a,10-hexahydro-2H-1-oxa-4a,8a-diaza-anthracene-7-carboxylic acid 2,4-difluoro-benylamide;1172581-47-3
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CAS No:
Description
Dolutegravir is a second-generation HIV integrase strand transfer inhibitor (INSTI) with an IC50 of 2.7 nM.
Characteristics
99.2
2.4
White to Pale Yellow Solid
1.53 g/cm3
190-193ºC
669.0±55.0°C at 760 mmHg
358.4±31.5 °C
1.650
In water, 95 mg/L at 25 deg C (est)
Store at 25 deg C (77 deg F); excursions permitted 15 deg to 30 deg C (59 deg to 86 deg F)
1.39X10-17 mm Hg at 25 deg C (est)
8.2None
Dolutegravir Use and Manufacturing
Dolutegravir is a second generation HIV-1 integrase strand transfer inhibitor. Dolutegravir is currently in Phase III clinical trials for the treatment of HIV infection. Dolutegravir has been shown to potently inhibit HIV replication in cells such as peripheral blood mononuclear cells (PBMCs), MT-4 cells and CIP4 cells infected with a self-inactivating PHIV lentiviral vector.
Drug Function and Efficacy
Inhibits HIV integrase by binding to the integrase active site and blocking the strand transfer step of reverse transcribed deoxyribonucleic acid (DNA) integration, a key step in the HIV replication cycle
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