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S/GSK1349572

Cat. No. M1718

S/GSK1349572 Structure

Synonym: GSK1349572, Dolutegravir

Size Price Availability Quantity
10mg USD 160 In stock
50mg USD 620 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

S/GSK1349572 (GSK1349572, Dolutegravir) is a novel potent inhibitor of HIV integrase  with an IC50 of 2.7 nM in vitro. Dolutegravir (DTG, GSK1349572) is metabolized primarily by uridine diphosphate glucuronyltransferase (UGT)1A1, with a minor role of cytochrome P450 (CYP)3A, and with renal elimination of unchanged compound being extremely low (< 1% of the dose). S/GSK1349572 is a next generation integrase inhibitor (INI) with low nM potency. Susceptibility to S/GSK1349572 and raltegravir (RAL) was determined for INI resistant clinical isolates from therapy experienced patients treated with RAL plus optimized background regimen.

Protocol
Cell Experiment
Cell lines MT-4 cells
Preparation method Antiviral assay in MT-4 cells. MT-4 cells growing exponentially at a density of 5 × 105 or 6 × 105/ml were 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 were then aliquoted to 96-well plates in the presence of varying concentrations of compounds. After incubation for 4 or 5 days, antiviral activity was determined by a cell viability assay that either measured bioluminescence with a CellTiter-Glo luminescent reagent (Promega Corporation, Madison, WI) or measured absorbance at 560 and 690 nm using the yellow tetrazolium MTT reagent [3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyltetrazolium bromide].
Concentrations 0.16, 0.8, 4, 20nM
Incubation time 4 or 5 days
Animal Experiment
Animal models unknow
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 305.28
Formula C20H19F2N3O5
CAS Number 900515-16-4
Purity >99%
Solubility DMSO 60 mg/mL
Storage at -20°C
References

Cross-resistance profile of the novel integrase inhibitor Dolutegravir (S/GSK1349572) using clonal viral variants selected in patients failing raltegravir.
Canducci et al. J Infect Dis. 2011 Dec 1;204(11):1811-5. PMID: 21984737.

Dolutegravir (S/GSK1349572) exhibits significantly slower dissociation than raltegravir and elvitegravir from wild-type and integrase inhibitor-resistant HIV-1 integrase-DNA complexes.
Hightower et al. Antimicrob Agents Chemother. 2011 Oct;55(10):4552-9. PMID: 21807982.

Structural and functional analyses of the second-generation integrase strand transfer inhibitor dolutegravir (S/GSK1349572).
Hare et al. Mol Pharmacol. 2011 Oct;80(4):565-72. PMID: 21719464.

Pharmacokinetics of the HIV integrase inhibitor S/GSK1349572 co-administered with acid-reducing agents and multivitamins in healthy volunteers.
Patel et al. J Antimicrob Chemother. 2011 Jul;66(7):1567-72. PMID: 21493648.

Prevalence of resistance mutations related to integrase inhibitor S/GSK1349572 in HIV-1 subtype B raltegravir-naive and -treated patients.
Malet et al. J Antimicrob Chemother. 2011 Jul;66(7):1481-3. PMID: 21474479.

Related Integrase Products
Dolutegravir

S/GSK1349572 (GSK1349572) is a two-metal-binding HIV integrase inhibitor with IC50 of 2.7 nM, modest activity against raltegravir-resistant signature mutants Y143R, Q148K, N155H, and G140S/Q148H.

MK-2048

MK-2048 is a potent inhibitor of integrase (IN) and INR263K with IC50 of 2.6 nM and 1.5 nM, respectively.

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.

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: S/GSK1349572, GSK1349572, Dolutegravir supplier, Integrase, inhibitors

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