Loading... Please wait...

Categories

Our Newsletter


GSK1349572 (Dolutegravir) | HIV integrase inhibitor

  • GSK1349572 (Dolutegravir).jpg
  • GSK1349572 (Dolutegravir), 400x400px, png
Price:
$159.00
Catalog #:
C4134-2s
Quantity:


Product Description

GSK1349572, a novel tricyclic-core containing inhibitor, has an IC50 of 2.7 nM against HIV-1 with a corresponding EC50s of 0.51 nM, 0.71 nM, and 2.2 nM in PBMCs, MT-4 cells, and PHIV assays, respectively. [1] Cytotoxic concentration (CC50) in unstimulated and stimulated PBMCs was 189 uM and 52 uM, which results in a selectivity index of 9400. Though similar in potency to first-generation integrase inhibitors, Raltegravir and Elvitegravir, GSK1349572 possesses and resistance profile that is markedly different. In cross-resistance profiling experiments, GSK1349572 showed efficacy against five non-nucleoside- and nucleoside- reverse transcriptase inhibitor-resistant viruses equal to that of wild-type virus (EC50 = 1.3 to 2.1 nM). Similarly, GSK1349572 was efficacious against two protease inhibitor-resistant viruses, again equivalent to activity against wild-type virus (EC50 = 0.36 and 0.37 nM).

In studies of clinical isolates from HIV-2-infected patients, the median EC50 value for GSK1349572 was found to be 0.8 nM. [2]


Technical information:

Chemical Formula:   C20H19F2N3O5
CAS #:   1051375-16-6
Molecular Weight:   419.38
Purity: > 98%
Appearance:   White
Chemical Name:   2H-Pyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazine-9-carboxamide, N-[(2,4-difluorophenyl)methyl]-3,4,6,8,12,12a-hexahydro-7-hydroxy-4-methyl-6,8-dioxo-, (4R,12aS)
Solubility:   Up to 100 mM in DMSO
Synonyms:   GSK1349572, S/GSK1349572, Dolutegravir

Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.


Reference:

1. Kobayashi et al., In Vitro Antiretroviral Properties of S/GSK1349572, a Next-Generation HIV Integrase Inhibitor. Antimicrob. Agents. Chemother. 2011, 55(2), 813-821. Pubmed ID: 21115794
2. Charpentier et al., In vitro phenotypic susceptibility of HIV-2 clinical isolates to the integrase inhibitor S/GSK1349572. AIDS, 2010, 24, 2753-2755. Pubmed ID: 20827161

Other Information:

Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.

Write your own product review

Product Reviews

This product hasn't received any reviews yet. Be the first to review this product!

Add to Wish List

Click the button below to add the GSK1349572 (Dolutegravir) | HIV integrase inhibitor to your wish list.

You Recently Viewed...