Dolutegravir (GSK1349572) - CAS 1051375-16-6
Catalog number: B0084-438457
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C20H19F2N3O5
Molecular Weight:
419.38
COA:
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Targets:
HIV
Description:
Dolutegravir (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.
Ordering Information
Catalog Number Size Price Stock Quantity
B0084-438457 25 mg $298 In stock
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Purity:
>98%
Synonyms:
S/GSK1349572
MSDS:
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InChIKey:
RHWKPHLQXYSBKR-BMIGLBTASA-N
InChI:
InChI=1S/C20H19F2N3O5/c1-10-4-5-30-15-9-24-8-13(17(26)18(27)16(24)20(29)25(10)15)19(28)23-7-11-2-3-12(21)6-14(11)22/h2-3,6,8,10,15,27H,4-5,7,9H2,1H3,(H,23,28)/t10-,15+/m1/s1
Canonical SMILES:
CC1CCOC2N1C(=O)C3=C(C(=O)C(=CN3C2)C(=O)NCC4=C(C=C(C=C4)F)F)O
1.Dolutegravir: an exciting new kid on the block.
Blanco Arévalo JL1, Whitlock GG. Expert Opin Pharmacother. 2014 Mar;15(4):573-82. doi: 10.1517/14656566.2014.868883. Epub 2014 Jan 22.
INTRODUCTION: Dolutegravir is the first second-generation integrase inhibitor approved for the treatment of naïve as well as experienced HIV-infected individuals.
2.Dolutegravir, a second-generation integrase inhibitor for the treatment of HIV-1 infection.
Rathbun RC1, Lockhart SM, Miller MM, Liedtke MD. Ann Pharmacother. 2014 Mar;48(3):395-403. doi: 10.1177/1060028013513558. Epub 2013 Nov 19.
OBJECTIVE: To review the pharmacology, safety, and efficacy of dolutegravir, an integrase strand-transfer inhibitor (INSTI), and to discuss its role in the treatment of HIV-1-infected patients.
3.Dolutegravir plus abacavir-lamivudine for the treatment of HIV-1 infection.
Walmsley SL, Antela A, Clumeck N, Duiculescu D, Eberhard A, Gutiérrez F, Hocqueloux L, Maggiolo F, Sandkovsky U, Granier C, Pappa K, Wynne B, Min S, Nichols G; SINGLE Investigators. N Engl J Med. 2013 Nov 7;369(19):1807-18. doi: 10.1056/NEJMoa1215541.
BACKGROUND: Dolutegravir (S/GSK1349572), a once-daily, unboosted integrase inhibitor, was recently approved in the United States for the treatment of human immunodeficiency virus type 1 (HIV-1) infection in combination with other antiretroviral agents. Dolutegravir, in combination with abacavir-lamivudine, may provide a simplified regimen.
4.Dolutegravir: a new integrase strand transfer inhibitor for the treatment of HIV.
Shah BM1, Schafer JJ, Desimone JA Jr. Pharmacotherapy. 2014 May;34(5):506-20. doi: 10.1002/phar.1386. Epub 2013 Dec 18.
The first two integrase strand transfer inhibitors (INSTIs) approved for treatment of patients infected with human immunodeficiency virus (HIV) were raltegravir and elvitegravir. Both raltegravir and elvitegravir are now guideline-preferred agents as part of an antiretroviral regimen for treatment-naive patients. However, raltegravir is dosed twice/day. Elvitegravir is available in a single-tablet regimen and dosed once/day because it is administered with the pharmacokinetic booster cobicistat, a potent CYP3A4 inhibitor that can lead to clinically significant drug-drug interactions. In addition, raltegravir and elvitegravir have a low genetic barrier to resistance and are associated with cross-resistance. Dolutegravir is a new-generation INSTI administered once/day without a pharmacokinetic booster and can be coformulated in a single-tablet regimen. Phase III studies have demonstrated the efficacy and safety of dolutegravir for treatment-naive and treatment-experienced patients.
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CAS 1051375-16-6 Dolutegravir (GSK1349572)

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