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Dolutegravir sodium

🥰Excellent
Catalog No. T2329Cas No. 1051375-19-9
Alias GSK-1349572A, GSK1349572

Dolutegravir sodium (GSK-1349572A) salt(DTG; GSK1349572) is an HIV integrase inhibitor(IC50: 2.7 nM), modest activity against raltegravir-resistant signature mutants Y143R, Q148K, N155H, and G140S/Q148H.

Dolutegravir sodium

Dolutegravir sodium

🥰Excellent
Purity: 99.46%
Catalog No. T2329Alias GSK-1349572A, GSK1349572Cas No. 1051375-19-9
Dolutegravir sodium (GSK-1349572A) salt(DTG; GSK1349572) is an HIV integrase inhibitor(IC50: 2.7 nM), modest activity against raltegravir-resistant signature mutants Y143R, Q148K, N155H, and G140S/Q148H.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$31In StockIn Stock
2 mg$44In StockIn Stock
5 mg$72In StockIn Stock
10 mg$113In StockIn Stock
25 mg$192In StockIn Stock
50 mg$247In StockIn Stock
100 mg$328In StockIn Stock
1 mL x 10 mM (in DMSO)$79In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.46%
Color:White to Yellow
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Product Introduction

Bioactivity
Description
Dolutegravir sodium (GSK-1349572A) salt(DTG; GSK1349572) is an HIV integrase inhibitor(IC50: 2.7 nM), modest activity against raltegravir-resistant signature mutants Y143R, Q148K, N155H, and G140S/Q148H.
Targets&IC50
HIV integrase:2.7 nM
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[1].
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[2].
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)
SynonymsGSK-1349572A, GSK1349572
Chemical Properties
Molecular Weight441.36
FormulaC20H18F2N3NaO5
Cas No.1051375-19-9
Smiles[Na+].C[C@@H]1CCO[C@H]2Cn3cc(C(=O)NCc4ccc(F)cc4F)c(=O)c([O-])c3C(=O)N12
Relative Density.no data available
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 4.42 mg/mL (10.01 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.2657 mL11.3286 mL22.6572 mL113.2862 mL
5 mM0.4531 mL2.2657 mL4.5314 mL22.6572 mL
10 mM0.2266 mL1.1329 mL2.2657 mL11.3286 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

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