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Dolutegravir

Cat. No. M3484

Dolutegravir Structure

Synonym: GSK1349572

Size Price Availability Quantity
5mg USD 160 In stock
10mg USD 240 In stock
50mg USD 600 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

S/GSK1349572 (GSK 1349572) is a novel potent integrase inhibitor with an IC50 of 2.7 nM in vitro. S/GSK1349572 (GSK 1349572) is a compound for the treatment of HIV infection. S/GSK1349572 (GSK 1349572) exhibited in vitro activity against most clinical isolates obtained from patients failing RAL-based therapy. In PBMC cell assay, S/GSK1349572 inhibited HIV integrase with the antiviral IC50=0.51 and IC90=2.0 nM. In MT-4 antiviral assays, potency shift extrapolated to 100% human serum was 75-fold providing PA-IC90=152 nM in PBMCs. S/GSK1349572 (GSK 1349572) had a markedly different resistance profile as evidenced by limited cross-resistance to RAL-resistant molecular clones, by its in vitro activity against clinical isolates obtained from patients failing RAL-based therapy, and in selecting different mutations with low level FC during serial passage. In vitro experiments support the potential for S/GSK1349572 (GSK 1349572) to have a higher genetic barrier to resistance when compared to 1st generation integrase inhibitors.

Protocol
Cell Experiment
Cell lines MT-4
Preparation method Growing MT-4 cells 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. Then aliquoting the cells to 96-well plates in the presence of varying concentrations of S/GSK1349572. After incubation for 4 or 5 days, using the yellow tetrazolium MTT reagent [3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyltetrazolium bromide] to determine antiviral activity by a cell viability assay that either measured bioluminescence with a CellTiter-Glo luminescent reagent or measured absorbance at 560 and 690 nm .
Concentrations 0 to 10 μM
Incubation time 4 days or 5 days
Animal Experiment
Animal models
Formulation
Dosages
Administration
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 419.38
Formula C20H19F2N3O5
CAS Number 1051375-16-6
Purity >99%
Solubility DMSO 80 mg/mL
Storage at -20°C
Related Integrase Products
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Raltegravir

Raltegravir (MK-0518) is a potent integrase (IN) inhibitor for WT and S217Q PFV IN with IC50 of 90 nM and 40 nM, respectively.

Elvitegravir

Elvitegravir (EVG) is a HIV integrase inhibitor with IC50 of 0.7 nM, 2.8 nM and 1.4 nM for HIV-1 IIIB, HIV-2 EHO and HIV-2 ROD, respectively.

S/GSK1349572

S/GSK1349572 (Dolutegravir) is a novel integrase inhibitor with an IC50 of 2.7 nM.

BMS-707035

BMS-707035 is an HIV-1 integrase (IN) inhibitor. HIV-1 integrase (IN) represents a therapeutically advantageous viral target to treat HIV/AIDS in the clinic.

  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Dolutegravir, GSK1349572 supplier, Integrase, inhibitors

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