Product Name

Dolutegravir

General description

Dolutegravir is a Human Immunodeficiency Virus Integrase Strand Transfer Inhibitor.

Synonym

(4R,12aS)-N-[(2,4-difluorophenyl)methyl]-7-hydroxy-4-methyl-6,8-dioxo-3,4,12,12a-tetrahydro-2H-pyrido[5,6]pyrazino[2,6-b][1,3]oxazine-9-carboxamide; GSK1349572

Purity

≥98.0%(HPLC)

CAS Number

1051375-16-6

Formula

C²⁰H¹⁹F²N³O⁵

Molecular Weight

419.38

Suitability

BioReagent,  suitable for cell culture, etc.

l  Physical and Chemical Information

Appearance

Solid

Solubility(25℃)

DMSO

≥50mg/mL(warmed)

Ethanol

Insoluble

Water

Insoluble

l  Biological Information

Biochem/Physiol  Actions

Dolutegravir is an orally bioavailable integrase strand-transfer inhibitor (INSTI), with activity against human immunodeficiency virus type 1 (HIV-1) infection. Upon oral administration, dolutegravir binds to the active site of integrase, an HIV enzyme that catalyzes the transfer of viral genetic material into human chromosomes. This prevents integrase from binding to retroviral deoxyribonucleic acid (DNA), and blocks the strand transfer step, which is essential for the HIV replication cycle. This prevents HIV-1. Dolutegravir is a two-metal-binding HIV integrase inhibitor with IC50 of 2.7 nM in a cell-free assay, modest activity against raltegravir-resistant signature mutants Y143R, Q148K, N155H, and G140S/Q148H.

l  Storage

Storage temp.

-20℃

l  Precautions and Disclaimer

This product is for R&D use only, not for drug, household, or other uses.

l  References

1.    http://www.drugbank.ca

2.    https://ncit.nci.nih.gov

3.    https://www.ncbi.nlm.nih.gov