- MK-2048
- Atazanavir
- Raltegravir (MK-0518)
- Elvitegravir (GS-9137)
- S/GSK1349572
| GSK744 (S/GSK1265744)HIV integrase inhibitor, oral active and long-acting |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
Science.2016 Aug 5;353(6299)594-8Nat Nanotechnol.2017 Dec;12(12):1190-1198.Nature Biotechnology.2017 Jun;35(6):569-576Nat Med.2018 Sep 17.Cell.2018 Dec 21. pii: S0092-8674(18)31561-7.Cell.Available online 25 October 2018.Cell.2018 Sep 27. pii: S0092-8674(18)31183-8.Cell.2018 Jun 28;174(1):172-186.e21.Cell.2018 Feb 22;172(5):1007-1021.e17.Cell.2017 Nov 30;171(6):1284-1300.e21.Cell.2017 Aug 17. pii: S0092-8674(17)30869-3.Cell.2017 Jul 13;170(2):312-323Nat Med.2018 Jan 29.Nat Med.2017 Nov;23(11):1342-1351.Cell.2017 Apr 6;169(2):286-300.Cell.2015 Aug 27;162(5):987-1002.Cell.2015 Feb 12;160(4):729-44.Nature Medicine.2017 Apr;23(4):493-500.Cancer Cell.2018 May 14;33(5):905-921.e5.Cancer Cell.2018 Apr 9;33(4):752-769.e8.Cancer Cell.2018 Mar 12;33(3):401-416.e8.Cancer Cell.2017 Aug 14;32(2):253-267.e5.Nat Methods.2018 Jul;15(7):523-526.Cell Stem Cell.2018 May 3;22(5):769-778.e4.Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Quality Control & MSDS
- View current batch:
- Purity = 99.65%
- COA (Certificate Of Analysis)
- HPLC
- NMR (Nuclear Magnetic Resonance)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
| Description | GSK744 is an oral and long-acting inhibitor of HIV integrase. | |||||
| Targets | HIV integrase | |||||
| IC50 | ||||||
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| Cas No. | 1051375-10-0 | SDF | Download SDF |
| Synonyms | GSK 744;GSK-744 | ||
| Chemical Name | (3S,11aR)-N-(2,4-difluorobenzyl)-6-hydroxy-3-methyl-5,7-dioxo-2,3,5,7,11,11a-hexahydrooxazolo[3,2-a]pyrido[1,2-d]pyrazine-8-carboxamide | ||
| Canonical SMILES | FC1=CC(F)=CC=C1CNC(C2=CN(C3=C(C2=O)O)C[C@H]4OC[C@H](C)N4C3=O)=O | ||
| Formula | C19H17F2N3O5 | M.Wt | 405.35 |
| Solubility | ≥19.35mg/mL in DMSO with gentle warming | Storage | Store at -20°C |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
GSK744 (S/GSK1265744) is a potential inhibitor of HIV integrase with IC50 value of 3 nM [1].HIV integrase is an enzyme produced by HIV virus that enables its genetic material to be integrated into the infected cell DNA. It is reported that HIV intergrase inhibitor plays an important role in halting HIV progression [2].GSK744 (S/GSK1265744) is a potent HIV integrase inhibitor. Using resistance passage experiments, integrase enzyme assays, and cellular assays with site-directed molecular (SDM) HIV clones resistant to other classes of anti-HIV-1 agents and earlier integrase strand transfer inhibitors, results showed that GSK1265744 efficiently inhibited HIV replication through inhibiting HIV integrase [1]. In female pigtail macaques model that intravaginal inoculated simian/human immunodeficiency virus twice a week for up to 11 weeks, GSK744 injection prevented the macaques from being infected by virus while placebo controls were infected after a 4 median vaginal challenges with SHIV which reminded that GSK744 may be a potential preexposure prophylaxis drug for prevention via inhibiting HIV integrase [3] [2].Many clinical trials have been conducted to show that GSK744 can efficiently protected healthy subjects from HIV infection [4-6].References: [1]. Yoshinaga, T., et al., Antiviral characteristics of GSK1265744, an HIV integrase inhibitor dosed orally or by long-acting injection. Antimicrob Agents Chemother, 2015. 59(1): p. 397-406.[2]. Andrews, C.D., et al., Long-acting integrase inhibitor protects macaques from intrarectal simian/human immunodeficiency virus. Science, 2014. 343(6175): p. 1151-4.[3]. Radzio, J., et al., The long-acting integrase inhibitor GSK744 protects macaques from repeated intravaginal SHIV challenge. Sci Transl Med, 2015. 7(270): p. 270ra5.[4]. Ford, S.L., et al., Lack of pharmacokinetic interaction between rilpivirine and integrase inhibitors dolutegravir and GSK1265744. Antimicrob Agents Chemother, 2013. 57(11): p. 5472-7.[5]. Spreen, W., et al., Pharmacokinetics, safety, and tolerability with repeat doses of GSK1265744 and rilpivirine (TMC278) long-acting nanosuspensions in healthy adults. J Acquir Immune Defic Syndr, 2014. 67(5): p. 487-92.[6]. Spreen, W.R., D.A. Margolis, and J.C. Pottage, Jr., Long-acting injectable antiretrovirals for HIV treatment and prevention. Curr Opin HIV AIDS, 2013. 8(6): p. 565-71.
