A potent inhibitor of HIV integrase (IC50 = 2.7 nM for HIV-1 integrase-catalyzed strand transfer in vitro); inhibits HIV-1 viral replication (EC50 = 0.51 nM) in PMBCs; CC50 values are 189 and 52 µM in unstimulated and stimulated PBMCs; prevents replication of several HIV-1 strains (EC50s = 0.36-2.1 nM) that are resistant to NRTIs

Dolutegravir – 10 mg

Brand:
Cayman
CAS:
1051375-16-6
Storage:
-20
UN-No:
Non-Hazardous - /

Dolutegravir is a potent inhibitor of HIV integrase with an IC50 value of 2.7 nM for HIV-1 integrase-catalyzed strand transfer in vitro.{40090} It inhibits HIV-1 viral replication (EC50 = 0.51 nM) in peripheral blood mononuclear cells (PBMCs). The cytotoxic concentration (CC50) values for dolutegravir in unstimulated and stimulated PBMCs are 189 and 52 µM, respectively, resulting in a therapeutic index of at least 9,400. It prevents replication of several HIV-1 strains (EC50s = 0.36-2.1 nM) that are resistant to nucleoside reverse transcriptase inhibitors (NRTIs), non-nucleoside reverse transcriptase inhibitors (NNRTIs), and protease inhibitors and impairs their ability to infect CIP4 cells.{40090,40091} Formulations containing dolutegravir have been used to treat HIV-1 infection in humans.{40092}  

 

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Description

A potent inhibitor of HIV integrase (IC50 = 2.7 nM for HIV-1 integrase-catalyzed strand transfer in vitro); inhibits HIV-1 viral replication (EC50 = 0.51 nM) in PMBCs; CC50 values are 189 and 52 µM in unstimulated and stimulated PBMCs; prevents replication of several HIV-1 strains (EC50s = 0.36-2.1 nM) that are resistant to NRTIs, NNRTIs, and protease inhibitors and impairs their ability to infect CIP4 cells

Formal name: (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

Synonyms:  GSK1349572|S/GSK1349572

Molecular weight: 419.4

CAS: 1051375-16-6

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Antivirals|Integrase Inhibitors||Product Type|Biochemicals|Small Molecule Inhibitors|Nucleic Acid Turnover/Signaling||Research Area|Immunology & Inflammation||Research Area|Infectious Disease|Viral Diseases|HIV & AIDS

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