Dolutegravir sodium

SKU: orb1305676

Description

Dolutegravir sodium

Research Area

Infectious Disease & Virology, Protein Biochemistry

Key Properties

• CAS Number: 1051375-19-9
• MW: 441.36
• Purity: 99.26%
• Formula: C₂₀H₁₈F₂N₃NaO₅
• SMILES: [Na+].C[C@@H]1CCO[C@H]2Cn3cc(C(=O)NCc4ccc(F)cc4F)c(=O)c([O-])c3C(=O)N12
• Target: HIV Protease
• Solubility: DMSO:4.42 mg/mL (10.01 mM)

Bioactivity

• Target IC50:
  HIV integrase:2.7 nM
• In Vivo:
  The bioavailability of dolutegravir was high when administered as a solution, but was limited by dissolution rate or solubility when administered as a suspension. Dolutegravir in the major circulating component in mice, rats, and monkeys, with Direct ether glucuronidation shown to b the Primary biotransformation pathway. Dolutegravir is primarily eliminated vi the feces either unabsorbed or by hydrolysis o the glucuronide or glucose conjugat.
• In Vitro:
  Dolutegravir(S/GSK1349572) inhibits HIV-1 integrase-catalyzed st and transfer with a 50% inhibitory concentration IC50 of 2.7 nM. S/GSK1349572 inhibits bot the HIV integration reaction st and transfer step in vitro and HIV replication in cells with similar potencies the inhibitor has no effect on total viral DNA synthesis in infected cells but block the integration of viral DNA into host DNA wit the same potency as its antiviral effec.
• Cell Research:
  In vitro growth Inhibition (cytotoxicity) studies are conducted with S/GSK1349572 in proliferating human leukemic and lymphomic cell lines (IM-9, U-937, MT-4, and Molt-4) as well as in stimulated and unstimulated human PBMCs. ATP levels are quantified by usin the CellTiter-Glo luciferase reagent to measure the ability of a compound to inhibit cell growth as an indicator o the compound's potential for cytotoxicity.(Only for Reference)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Disclaimer: For research use only

Alternative Names

GSK 1349572, GSK1349572, GSK-1349572, GSK-1349572A, HIV Integrase, HIV Protease, HIV, HIV integrase, HIVProtease, Inhibitor, Human immunodeficiency virus, inhibit, Dolutegravir, Dolutegravir sodium, S/GSK1349572

Compound Identifiers

PubChem CID

46216142