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.
