Dolutegravir
Dolutegravir
CAS: 1051375-16-6
Molecular Formula: C20H19F2N3O5
Dolutegravir - Names and Identifiers
| Name | Dolutegravir |
| Synonyms | Dolutegravir Dolutegravir API Dolutegravir free acid Dolutegravir (GSK1349572) GSK1349572, S-349572, GSK572 |
| CAS | 1051375-16-6 |
Dolutegravir - Physico-chemical Properties
| Molecular Formula | C20H19F2N3O5 |
| Molar Mass | 419.38 |
| Density | 1.53 |
| Melting Point | 187-189°C |
| Boling Point | 669.0±55.0 °C(Predicted) |
| Solubility | DMSO 84 mg/mL, water <1 mg/mL, ethanol <1 mg/mL |
| Appearance | White or yellowish solid |
| Color | White to Pale Beige |
| pKa | 4.50±1.00(Predicted) |
| Storage Condition | Refrigerator |
| MDL | MFCD20488027 |
| Use | This product is for scientific research only and shall not be used for other purposes. |
| In vitro study | S/GSK1349572 showed potent inhibitory effects against nine clinical isolates from patients infected with integrase inhibitor-natural HIV-2, with EC50 ranging from 0.2 nM to 1.4 nM. In Vitro, S/GSK1349572 inhibited strand transfer catalyzed by recombinant HIV-1 integrase with an IC50 of 2.7 nM. In addition, S/GSK1349572 effectively inhibits HIV replication in cells, such as peripheral blood mononuclear cells (PBMCs),MT-4 cells and CIP4 cells infected with self-inactivated PHIV lentiviral vectors, the EC50 was 0.51 nM,0.71 nM and 2.2 nM, respectively. In Vitro, S/GSK1349572 exhibited potent activity against five different non-nucleoside retroviral inhibitor resistant viruses, or nucleoside retroviral inhibitor resistant viruses, with an EC50 range of 1.3 nM -2.1 nM. Similar to the wild-type virus, S/GSK1349572 showed the same activity against both protease inhibitor resistant viruses with EC50 of 0.36 nM and 0.37 nM. |
Dolutegravir - Introduction
S/GSK1349572 (GSK1349572) is an HIV integrase inhibitor with IC50 of 2.7 nM. It acts moderately and effectively on anti-Raltegravir mutants Y143R, Q148K, N155H, and G140S/Q148H.
Last Update：2022-10-16 17:11:44
Dolutegravir - Reference Information
| overview | duluvir free acid (dolutegravir,DTG), trade name: TIVICAY) was approved by the U.S. Food and Drug Administration on August 12, 2013. it is a human immunodeficiency virus type 1(HIV-1) integrase chain transfer inhibitor (INSTI), it is suitable for the treatment of HIV-1 infection in adults and children over 12 years old and with a body mass of at least 40kg in combination with other antiretroviral drugs. |
| application | vutwe (dolutegravir,DTG), trade name: TIVICAY) was approved by the U.S. Food and Drug Administration on August 12, 2013. It is a human immunodeficiency virus type 1(HIV-1) integrase chain transfer inhibitor (INSTI), it is suitable for the treatment of HIV-1 infection in adults and children over 12 years old and with a body mass of at least 40kg in combination with other antiretroviral drugs. |
| new anti-AIDS drug | Du Rutway (Drogway, Dolutegravir,Tivicay) is a new anti-AIDS drug developed by 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. On August 12, 2013, the U.S. Food and Drug Administration (FDA) approved it for previously treated or newly treated HIV-1 adults and children aged 12 and above weighing at least 40kg. Dolutegravir is a drug taken once a day, which has achieved the same efficacy as Mercadon HIV/AIDS drug retgervir (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. Analysts expect Dolutegravir to become a blockbuster drug with billions of dollars in annual sales and a strong competitor to Gilead Sciences's Atripla of the world's best-selling HIV compound drugs. |
| biological activity | Dolutegravir (GSK1349572, S/GSK1349572) is a two-metal-bound HIV integrase inhibitor. IC50 is 2.7 nM in cell-free test. it has moderate activity against significant Raltegravir-resistant mutants Y143R,Q148K,N155H, and G140S/Q148H. |
| Target | Value |
| HIV integrase (Cell-free assay) | 2.7 nM |
| use | Dolutegravir (GSK1349572) is an HIV integrase inhibitor with IC50 of 2.7 nM. it acts moderately and effectively on significant mutants Y143R, Q148K, N155H, and G140S/Q148H that are anti-Raltegravir. |
| toxic substance data | information provided by: pubchem.ncbi.nlm.nih.gov (external link) |
Last Update：2024-04-09 20:52:54
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