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Dolutegravir

pharmaceutical raw materials
Dolutegravir structure

Dolutegravir 

structure
  • CAS No:

    1051375-16-6

  • Formula:

    C20H19F2N3O5

  • Chemical Name:

    Dolutegravir

  • 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

  • Categories:

    Biochemical Engineering  >  Inhibitors

Description

Dolutegravir is a second-generation HIV integrase strand transfer inhibitor (INSTI) with an IC50 of 2.7 nM.

Dolutegravir Basic Attributes

419.3787664

419.38

809-888-1

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

Safety Information

P273, P391, P501

H400

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

This ingredient has been used in drugs with the following functions (note: it does not mean that the ingredient itself has the following health functions)

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