WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 315142
CAS#: 1051375-16-6 (free)
Description: Dolutegravir, also known as GSK1349572, is a potent inhibitor of HIV integrase with an IC50 value of 2.7 nM for HIV-1 integrase-catalyzed strand transfer in vitro.1 It inhibits HIV-1 viral replication (EC50 = 0.51 nM) in peripheral blood mononuclear cells (PBMCs). Dolutegravir (DTG) is an antiretroviral medication used, together with other medication, to treat HIV/AIDS. It may also be used, as part of post exposure prophylaxis, to prevent HIV infection following potential exposure.
MedKoo Cat#: 315142
CAS#: 1051375-16-6 (free)
Chemical Formula: C20H19F2N3O5
Exact Mass: 419.12928
Molecular Weight: 419.38
Elemental Analysis: C, 57.28; H, 4.57; F, 9.06; N, 10.02; O, 19.08
Dolutegravir (GSK1349572), purity > 98%, is in stock. The same day shipping out after order is received.
Synonym: Dolutegravir; GSK1349572; GSK-1349572; GSK 1349572; Tivicay; S/GSK1349572.
IUPAC/Chemical Name: (4R,12aS)-N-(2,4-difluorobenzyl)-7-hydroxy-4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-pyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazine-9-carboxamide
InChi Key: RHWKPHLQXYSBKR-BMIGLBTASA-N
InChi Code: 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
SMILES Code: O=C(C1=CN(C2=C(O)C1=O)C[C@]3([H])OCC[C@@H](C)N3C2=O)NCC4=CC=C(F)C=C4F
The following data is based on the product molecular weight 419.38 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.15 mL||5.76 mL||11.51 mL|
|5 mM||0.23 mL||1.15 mL||2.3 mL|
|10 mM||0.12 mL||0.58 mL||1.15 mL|
|50 mM||0.02 mL||0.12 mL||0.23 mL|
1: Llibre JM, Clotet B. Once-daily single-tablet regimens: a long and winding road to excellence in antiretroviral treatment. AIDS Rev. 2012 Jul;14(3):168-78. PubMed PMID: 22833060.
2: Rhodes MC, Laffan S, Genell C, Gower J, Maier C, Fukushima T, Nichols G, Eaton Bassiri A. Assessing a Theoretical Risk of Dolutegravir-Induced Developmental Immunotoxicity in Juvenile Rats. Toxicol Sci. 2012 Jul 12. [Epub ahead of print] PubMed PMID: 22790968.
3: Adams JL, Greener BN, Kashuba AD. Pharmacology of HIV integrase inhibitors. Curr Opin HIV AIDS. 2012 Jul 19. [Epub ahead of print] PubMed PMID: 22789987.
4: Lennox JL. The use of HIV-1 integrase inhibitors in antiretroviral naive patients. Curr Opin HIV AIDS. 2012 Jul 19. [Epub ahead of print] PubMed PMID: 22789985.
5: Shamroe CL, Bookstaver PB, Rokas KE, Weissman SB. Update on raltegravir and the development of new integrase strand transfer inhibitors. South Med J. 2012 Jul;105(7):370-8. PubMed PMID: 22766666.
6: Saladini F, Meini G, Bianco C, Monno L, Punzi G, Pecorari M, Borghi V, Di Pietro M, Filice G, Gismondo MR, Micheli V, Penco G, Carli T, De Luca A, Zazzi M; for the ARCA Collaborative Group. Prevalence of HIV-1 integrase mutations related to resistance to dolutegravir in raltegravir naÃ¯ve and pretreated patients. Clin Microbiol Infect. 2012 May 28. doi: 10.1111/j.1469-0691.2012.03917.x. [Epub ahead of print] PubMed PMID: 22716970.
7: Quashie PK, Sloan RD, Wainberg MA. Novel therapeutic strategies targeting HIV integrase. BMC Med. 2012 Apr 12;10:34. Review. PubMed PMID: 22498430; PubMed Central PMCID: PMC3348091.
8: Nguyen HL, Ruxrungtham K, Delaugerre C. Genetic barrier to the development of resistance to integrase inhibitors in HIV-1 subtypes CRF01_AE and B. Intervirology. 2012;55(4):287-95. Epub 2012 Mar 23. PubMed PMID: 22456540.
9: Chen S, Min SS, Peppercorn A, Borland J, Lou Y, Song I, Fujiwara T, Piscitelli SC. Effect of a single supratherapeutic dose of dolutegravir on cardiac repolarization. Pharmacotherapy. 2012 Apr;32(4):333-9. doi: 10.1002/j.1875-9114.2012.01033.x. Epub 2012 Mar 15. PubMed PMID: 22422361.
10: Katlama C, Murphy R. Dolutegravir for the treatment of HIV. Expert Opin Investig Drugs. 2012 Apr;21(4):523-30. Epub 2012 Mar 2. Review. PubMed PMID: 22380682.
Dolutegravir, also known as GSK1349572, is an FDA-approved drug for the treatment of HIV infection. It can be used to treat HIV-infected adults who have never taken HIV therapy (treatment-naïve) and HIV-infected adults who have previously taken HIV therapy (treatment-experienced), including those who have been treated with other integrase strand transfer inhibitors. Tivicay is also approved for children ages 12 years and older weighing at least 40 kilograms (kg) who are treatment-naïve or treatment-experienced but have not previously taken other integrase strand transfer inhibitors.