CAS 1051375-16-6

Dolutegravir

Descrizione:

Dolutegravir è un farmaco antiretrovirale utilizzato principalmente nel trattamento dell'infezione da HIV. Appartiene alla classe di farmaci noti come inibitori del trasferimento della catena di integrasi (INSTIs), che agiscono bloccando l'enzima integrasi, impedendo l'integrazione del DNA virale nel genoma della cellula ospite. Dolutegravir è caratterizzato dalla sua alta potenza, dal profilo farmacocinetico favorevole e da una bassa barriera alla resistenza, rendendolo efficace in vari regimi di trattamento. La sostanza è tipicamente somministrata per via orale ed è ben assorbita, con una lunga emivita che consente una somministrazione una volta al giorno. Spesso è combinata con altri agenti antiretrovirali per migliorare l'efficacia e ridurre il rischio di resistenza. Dolutegravir è generalmente ben tollerato, anche se alcuni pazienti possono sperimentare effetti collaterali come insonnia, mal di testa o disturbi gastrointestinali. La sua struttura chimica include un nucleo biciclico, contribuendo al suo meccanismo d'azione e stabilità. In generale, Dolutegravir rappresenta un avanzamento significativo nella terapia dell'HIV, migliorando i risultati del trattamento per molti pazienti.

Formula: C₂₀H₁₉F₂N₃O₅

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

InChI key: InChIKey=RHWKPHLQXYSBKR-BMIGLBTASA-N

SMILES: O=C1C=2N(C[C@]3(N1[C@H](C)CCO3)[H])C=C(C(NCC4=C(F)C=C(F)C=C4)=O)C(=O)C2O

Sinonimi:

• (4R,12aS)-N-[(2,4-Difluorophenyl)methyl]-3,4,6,8,12,12a-hexahydro-7-hydroxy-4-methyl-6,8-dioxo-2H-pyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazine-9-carboxamide
• (4R,12aS)-N-[(2,4-Difluorophenyl)methyl]-3,4,6,8,12,12a-hexahydro-7-hydroxy-4-methyl-6,8-dioxo-2H-pyrido[1′,2′:4,5]pyrazino[2,1-b][1,3]oxazine-9-carboxamide
• (4R,9aS)-5-Hydroxy-4-methyl-6,10-dioxo-3,4,6,9,9a,10-hexahydro-2H-1-oxa-4a,8a-diaza-anthracene-7-carboxylic acid 2,4-difluoro-benylamide
• 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)-
• Dolutegravir free acid
• Gsk 1349572
• Gsk1349572
• S/Gsk1349572
• Soltegravir
• Tivicay
• Dolutegravir

Dolutegravir

CAS: 1051375-16-6

Dolutegravir

Purezza: ≥98%

Peso molecolare: 419.38g/mol

Ref: 54-BUP15005

(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

CAS: 1051375-16-6

(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

Purezza: 98%

Peso molecolare: 419.38g/mol

Ref: 54-PC109099

Dolutegravir

CAS: 1051375-16-6

Formula: C₂₀H₁₉F₂N₃O₅

Colore e forma: White To Off-White Solid

Peso molecolare: 419.38

Ref: 4Z-D-093001

Dolutegravir-d5

CAS: 1051375-16-6

Formula: C₂₀H₁₄D₅F₂N₃O₅

Colore e forma: Off-White Solid

Peso molecolare: 424.42

Ref: 4Z-D-093002

Dolutegravir-d6

CAS: 1051375-16-6

Formula: C₂₀H₁₃D₆F₂N₃O₅

Peso molecolare: 425.42

Ref: 4Z-D-093045

Dolutegravir

CAS: 1051375-16-6

Dolutegravir (GSK1349572), HIV integrase inhibitor with IC50 of 2.7 nM, partly effective against some raltegravir-resistant HIV strains.

Formula: C₂₀H₁₉F₂N₃O₅

Purezza: 98.97% - 99.75%

Colore e forma: White To Pale Yellow Solid

Peso molecolare: 419.38

Ref: TM-T6198

Dolutegravir

CAS: 1051375-16-6

Applications Dolutegravir is a second generation HIV-1 integrase strand transfer inhibitor. Dolutegravir is currently in Phase III clinical trials for the treatment of HIV infection. Dolutegravir has been shown to potently inhibit HIV replication in cells such as peripheral blood mononuclear cells (PBMCs), MT-4 cells and CIP4 cells infected with a self-inactivating PHIV lentiviral vector.
References Kobayashi, M. et al. Antimicrob Agents Chemother., 55, 813 (2011); Garrido, C. et al.: Antiviral, Res., 90, 164 (2011); Lenz, J.C.C. et al.: Exp. Opin. Invest. Drugs, 20, 537 (2011);

Formula: C₂₀H₁₉F₂N₃O₅

Colore e forma: White To Beige

Peso molecolare: 419.38

Ref: TR-D528800

Dolutegravir-d4

Prodotto controllato

CAS: 1051375-16-6

Applications Isotope labelled Dolutegravir is a second generation HIV-1 integrase strand transfer inhibitor. Dolutegravir is currently in Phase III clinical trials for the treatment of HIV infection. Dolutegravir has been shown to potently inhibit HIV replication in cells such as peripheral blood mononuclear cells (PBMCs), MT-4 cells and CIP4 cells infected with a self-inactivating PHIV lentiviral vector.
References Kobayashi, M. et al. Antimicrob Agents Chemother., 55, 813 (2011); Garrido, C. et al.: Antiviral, Res., 90, 164 (2011); Lenz, J.C.C. et al.: Exp. Opin. Invest. Drugs, 20, 537 (2011);

Formula: C₂₀H₁₅D₄F₂N₃O₅

Purezza: >80%

Colore e forma: Neat

Peso molecolare: 423.4

Ref: TR-D528802

Dolutegravir

CAS: 1051375-16-6

Dolutegravir is an HIV-1 integrase inhibitor. Dolutegravir is used in the treatment of HIV-1 infections as it hampers the integration of the viral genome into the host DNA (Katlama, 2012). Active on a wide number of HIV-1 phenotypes, dolutegravir is highly bioavailable with an IC90 of more than 30 hours (Cottrell, 2013).

Formula: C₂₀H₁₉F₂N₃O₅

Purezza: Min. 98 Area-%

Colore e forma: White Powder

Peso molecolare: 419.40 g/mol

Ref: 3D-FD43372

Dolutegravir

CAS: 1051375-16-6

Purezza: 98%

Peso molecolare: 419.385

Ref: 10-F799806

Dolutegravir (0.1 mg/mL in Methanol)

CAS: 1051375-16-6

Formula: C₂₀H₁₉F₂N₃O₅

Colore e forma: Colourless

Peso molecolare: 419.38

Ref: TR-KIT7755