Dolutegravir sodium

SKU: orb1305676

Description

Dolutegravir sodium (DTG) is a potent HIV integrase inhibitor (IC50: 2.7 nM) with activity against several raltegravir-resistant mutants. It is widely used in antiviral research for in vitro mechanistic studies and in vivo models of HIV infection, supporting the development of next-generation antiretroviral therapies.

Research Area

Infectious Disease & Virology, Protein Biochemistry

Images & Validation

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Key Properties

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CAS Number	1051375-19-9
MW	441.36
Purity	99.74% (May vary between batches)
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

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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 is the major circulating component in mice, rats, and monkeys, with direct ether glucuronidation shown to be the primary biotransformation pathway. Dolutegravir is primarily eliminated via the feces either unabsorbed or by hydrolysis of the glucuronide or glucose conjugate. Read more...
In Vitro	Dolutegravir(S/GSK1349572) inhibits HIV-1 integrase-catalyzed strand transfer with a 50% inhibitory concentration (IC50) of 2.7 nM. S/GSK1349572 inhibits both the HIV integration reaction strand 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 blocks the integration of viral DNA into host DNA with the same potency as its antiviral effect. Read more...
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 using the CellTiter-Glo luciferase reagent to measure the ability of a compound to inhibit cell growth as an indicator of the compound's potential for cytotoxicity.(Only for Reference) Read more...

Storage & Handling

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Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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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

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Compound Identifiers

PubChem CID

46216142 ↗

Key Properties

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No computed properties available.

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