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Dolutegravir

Catalog No. T6198 CAS 1051375-16-6

Synonyms: S/GSK1349572, GSK1349572

Dolutegravir (GSK1349572) (IC50=2.7 nM), a two-metal-binding HIV integrase inhibitor, exhibits medium activity against raltegravir-resistant signature mutants Y143R, Q148K, N155H, and G140S/Q148H.

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Dolutegravir, CAS 1051375-16-6

Pack Size	Availability	Price/USD
1 mg	In stock	$ 30.00
2 mg	In stock	$ 43.00
5 mg	In stock	$ 68.00
10 mg	In stock	$ 117.00
25 mg	In stock	$ 180.00
50 mg	In stock	$ 288.00
100 mg	In stock	$ 450.00
200 mg	In stock	$ 638.00
500 mg	In stock	$ 895.00
1 g	In stock	$ 1,170.00
1 mL * 10 mM (in DMSO)	In stock	$ 63.00

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Purity: 99.08%

Purity: 99.05%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Dolutegravir (GSK1349572) (IC50=2.7 nM), a two-metal-binding HIV integrase inhibitor, exhibits medium activity against raltegravir-resistant signature mutants Y143R, Q148K, N155H, and G140S/Q148H.
Targets&IC50	HIV integrase:2.7 nM
In vitro	S/GSK1349572 shows the potent inhibitory effect on nine clinical isolates from integrase inhibitor-naive HIV-2-infected patients with EC50 ranging from 0.2 nM -1.4 nM. [1] In vitro, S/GSK1349572 inhibits recombinant HIV-1 integrase-catalyzed strand transfer with IC50 of 2.7 nM. Furthermore, S/GSK1349572 potently inhibits 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 with EC50 of 0,51 nM, 0.71 nM and 2.2 nM, respectively. [2] In vitro, S/GSK1349572 exhibits potent activity against five different nonnucleoside reverse transcription inhibitor--resistant or nucleoside reverse transcription inhibitor--resistant viruses with EC50 ranging from 1.3 nM -2.1 nM. Similarly to that against wild-type virus, S/GSK1349572 shows equivalent activity against two protease inhibitor-resistant viruses with EC50 of 0.36 nM and 0.37 nM, respectively. [2]
In vivo	Following a single intravenous (IV) administration, Dolutegravir exhibits low plasma clearance rates in both rats (0.23 mL/min/kg) and monkeys (2.12 mL/min/kg), with a similar half-life of approximately 6 hours and a low steady-state volume of distribution (VSS) in both species. When administered orally as a solution to fasted male rats and a single monkey, Dolutegravir is rapidly absorbed, demonstrating high oral bioavailability (75.6% and 87.0%, respectively). Additionally, Dolutegravir exposure, measured by peak concentration (Cmax) and area under the curve (AUC), increases with dose escalation in oral suspension forms up to 250 mg/kg in non-fasted rats and up to 50 mg/kg in non-fasted monkeys, albeit with a less than proportional rise[3].
Kinase Assay	In vitro strand transfer assay: The inhibitory potencies of S/GSK1349572 and other INIs are measured in a strand transfer assay using recombinant HIV integrase. A complex of integrase and biotinylated preprocessed donor DNA-streptavidin-coated Acintillation proximity assay (SPA) beads is formed by incubating 2 μM purified recombinant integrase with 0.66 μM biotinylated donor DNA-4 mg/mL streptavidin-coated SPA beads in 25 mM sodium morpholinepropanesulfonic acid (MOPS) (pH 7.2), 23 mM NaCl, and 10 mM MgCl2 for 5 minutes at 37 °C. These beads are spun down and preincubated with diluted INIs for 60 minutes at 37 °C. Then a 3H-labeled target DNA substrate is added to give a final concentration of 7 nM substrate, and the strand transfer reaction mixture is incubated at 37 °C for 25 to 45 minutes, which allows for a linear increase in the strand transfer of donor DNA to radiolabeled target DNA. The signal is read using a Wallac MicroBeta scintillation plate reader.
Cell Research	MT-4 cells growing exponentially at a density of 500000 or 600000 /mL are infected with HIV-1 strain IIIB at a viral multiplicity of infection of 0.001 or a 50% tissue culture infective dose of 4 to 10. The cells are then aliquoted to 96-well plates in the presence of varying concentrations of S/GSK1349572. After incubation for 4 or 5 days, antiviral activity is determined by a cell viability assay that either measured bioluminescence with a CellTiter-Glo luminescent reagent or measured absorbance at 560 and 690 nm using the yellow tetrazolium MTT reagent [3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyltetrazolium bromide]. (Only for Reference)

Synonyms	S/GSK1349572, GSK1349572
Molecular Weight	419.38
Formula	C20H19F2N3O5
CAS No.	1051375-16-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 77 mg/mL (183.6 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

1. Charpentier C, et al. AIDS. 2010, 24(17), 2753-275 2. Kobayashi M, et al. Antimicrob Agents Chemother. 2011, 55(2), 813-821. 3. Moss L, et al. The comparative disposition and metabolism of dolutegravir, a potent HIV-1 integrase inhibitor, in mice, rats, and monkeys. Xenobiotica. 2015 Jan;45(1):60-70. 4. Herrmann A, Roesner M, Werner T, et al. Potent inhibition of HIV replication in primary human cells by novel synthetic polyketides inspired by Aureothin[J]. Scientific Reports. 2020, 10(1): 1-15.

Citations

1. Herrmann A, Roesner M, Werner T, et al. Potent inhibition of HIV replication in primary human cells by novel synthetic polyketides inspired by Aureothin. Scientific Reports. 2020, 10(1): 1-15

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Drug Repurposing Compound Library EMA Approved Drug Library FDA-Approved Drug Library Clinical Compound Library Immunology/Inflammation Compound Library NO PAINS Compound Library Drug-induced Liver Injury (DILI) Compound Library FDA-Approved & Pharmacopeia Drug Library Bioactive Compound Library

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Keywords

Dolutegravir 1051375-16-6 Microbiology/Virology Proteases/Proteasome HIV Protease GSK 1349572 S/GSK1349572 HIV Integrase GSK-1349572 HIV inhibit S/GSK-1349572 S/GSK 1349572 GSK1349572 Human immunodeficiency virus Inhibitor inhibitor

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