Dolutegravir sodium salt
Dolutegravir sodium salt;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-, sodium salt
CAS: 1051375-19-9
Molecular Formula: C20H20F2N3NaO5
Dolutegravir sodium salt - Names and Identifiers
| Name | Dolutegravir sodium salt 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-, sodium salt |
| Synonyms | GSK 1349572A DOLUTEGRAVIR SODIUM GSK1349572 sodiuM salt Dolutegravir sodiuM salt Dolutegravir sodium salt Dolutegravir SodiuM ( API) Dolutegravir sodium(GSK1349572) |
| CAS | 1051375-19-9 |
| EINECS | 812-620-6 |
Dolutegravir sodium salt - Physico-chemical Properties
| Molecular Formula | C20H20F2N3NaO5 |
| Molar Mass | 443.38 |
| Melting Point | >300oC |
| Solubility | DMSO: ≥ 4.4 mg/mL; DMSO: < 12.6 mg/mL |
| Appearance | Solid |
| Color | White to Green |
| Storage Condition | Hygroscopic, -20°C Freezer, Under inert atmosphere |
| Stability | Hygroscopic |
| In vitro study | Dolutegravir(S/GSK1349572) inhibits chain transfer catalyzed by HIV integrase with an IC50 of 2.7 nM. S/GSK1349572 inhibits both the HIV integration reaction chain transfer step and HIV replication in vitro. While it had no effect on total viral DNA synthesis in infected cells, it prevented the integration of viral DNA into host DNA. |
| In vivo study | The bioavailability of dolutegravir is high when administered as a solution, but is limited by its dissolution or solubility when administered as a suspension. Dolutegravir is a major circulating component in mice, rats and monkeys, and its main biotransformation pathway is direct ether sugar esterification. The elimination of Dolutegravir in the body is mainly through the hydrolysis of the covalent complex of glucuronide or glucose and the excretion of excretions. |
Dolutegravir sodium salt - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.266 ml | 11.329 ml | 22.657 ml |
| 5 mM | 0.453 ml | 2.266 ml | 4.531 ml |
| 10 mM | 0.227 ml | 1.133 ml | 2.266 ml |
| 5 mM | 0.045 ml | 0.227 ml | 0.453 ml |
Last Update：2024-01-02 23:10:35
Dolutegravir sodium salt - Reference Information
| Use | Duluvir sodium salt is the second generation of HIV-1 integrase chain transfer inhibitors. Duluvir sodium salt is currently in a phase III clinical trial for the treatment of HIV infection. Duluvir sodium has been shown to be effective in inhibiting HIV replication in cells infected with self-inactivating PHIV lentiviral vectors, such as peripheral blood mononuclear cells (PBMC),MT-4 cells and CIP4 cells. |
| application | August 12, 2013 approved by the U.S. food and drug administration (FDA) for previously treated or newly treated adults and children aged 12 and above weighing at least 40kg. Dolutegravir is a once-a-day drug that has achieved comparable efficacy to Mercadon's HIV/AIDS drug Retegivir (Raltegravir,Isentress) in phase III clinical trials. Retegweir was taken twice, both of which were inhibitors of HIV integrase. FDA officials said that people infected with AIDS need targeted treatment according to their specific conditions, and the Tivicay will provide patients with new choices. In a study conducted a year ago, after 48 weeks of Tivicay treatment, 88% of patients had significantly improved their condition, which was better than Gilead's Atripla. |
| Du Rutway | Du Rutway (Drogway, Dolutegravir,Tivicay) is a new anti-AIDS drug developed by the British pharmaceutical giant GlaxoSmithKline (GSK) and Japan's Shiano Pharmaceutical Company (Shionogi). In July 2012, Gelansu SmithKline Pharmaceutical Company and Japan Shiano Yoshiki Pharmaceutical Company announced the results of the Phase III clinical trial of the new AIDS drug Dolutegravir. After 48 weeks of treatment with dolutegravir drugs and two other old AIDS drugs, the patient's body 88% The virus was successfully suppressed, after taking Gilead Sciences's three-in-one oral drug Atripla (according to Weenz/emtricitabine/tenofovir fumarate tablets, Efavirenz/Emtricitabine /Tenofovir Disoproxil Fumarate), the virus 81% in the patient's body is suppressed, which shows that GlaxoSmithKline's dolutegravir drugs are slightly better. According to the researchers, in the comparison test, due to the side effects of the drug, 10% of the patients finally stopped taking Atripla drugs of Gilead Technology, but only 2% of the patients stopped taking dolutegravir drugs of GlaxoSmithKline Pharmaceutical Company, which shows that the safety of GlaxoSmithKline dolutegravir drugs is slightly higher. |
| biological activity | Dolutegravir Sodium (GSK-1349572A) is an HIV integrase inhibitor with IC50 of 2.7 nM. |
| Target | Value |
| HIV integrase (Cell-free assay) | 2.7 nM |
Last Update：2024-04-09 02:00:05
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