| GSK1349572 sodiuM saltNext-generation HIV integrase (IN) inhibitor |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
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- Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
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Chemical structure
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| Cas No. | 1051375-19-9 | SDF | Download SDF |
| Synonyms | N/A | ||
| Chemical Name | sodium (4R,12aS)-9-((Z)-((2,4-difluorobenzyl)imino)(hydroxy)methyl)-4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-pyrido[1",2":4,5]pyrazino[2,1-b][1,3]oxazin-7-olate | ||
| Canonical SMILES | C[C@](N12)([H])CCO[C@@]1([H])CN(C(C2=O)=C3[O-])C=C(/C(O)=N/CC4=C(F)C=C(F)C=C4)C3=O.[Na+] | ||
| Formula | C20H18F2N3NaO5 | M.Wt | 441.36 |
| Solubility | ≥8.06mg/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. | ||
Integrase inhibitors are a new class of antiretroviral drugs blocking the action of HIV integrase, which catalyses several key steps in the life cycle of the virus and is essential for insertion of the viral genome into the host cell DNA. GSK1349572 is a next-generation HIV integrase (IN) inhibitor.
In vitro: GSK1349572 is a two-metal-binding HIV integrase strand transfer inhibitor whose mechanism of action was established through resistance passage experiments, integrase enzyme assays, mechanistic cellular assays and activity against viral strains resistant to other classes of anti-HIV agents. In a variety of cellular antiviral assays, GSK1349572 inhibited HIV replication with subnanomolar or low-nanomolar potency and with a selectivity index of 9,400. The protein-adjusted half-maximal effective concentration extrapolated to 100% human serum was 38 nM [1].
In vivo: No animial in vivo data are available for GSK1349572 so far.
Clinical trial: GSK1349572 was effective when given once daily without a pharmacokinetic booster and was well tolerated at all assessed doses. These findings support the assessment of once daily 50 mg GSK1349572 in phase 3 trials.
Reference:[1] Kobayashi M, Yoshinaga T, Seki T, Wakasa-Morimoto C, Brown KW, Ferris R, Foster SA, Hazen RJ, Miki S, Suyama-Kagitani A, Kawauchi-Miki S, Taishi T, Kawasuji T, Johns BA, Underwood MR, Garvey EP, Sato A, Fujiwara T. In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor. Antimicrob Agents Chemother. 2011 Feb;55(2):813-21. [2] van Lunzen J, Maggiolo F, Arribas JR, Rakhmanova A, Yeni P, Young B, Rockstroh JK, Almond S, Song I, Brothers C, Min S. Once daily dolutegravir (S/GSK1349572) in combination therapy in antiretroviral-naive adults with HIV: planned interim 48 week results from SPRING-1, a dose-ranging, randomised, phase 2b trial. Lancet Infect Dis. 2012 Feb;12(2):111-8.
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RACE是基于PCR技术基础上由已知的一段cDNA片段，通过往两端延伸扩增从而获得完整的3'端和5'端的方法
RACE技术的原理和操作方法：http://wenku.baidu.com/link?url=J-9lPSGmRLQriSfXhOqcYYFvJx7ktGIRMgU6k9vDQIywtdJ8deNg7Qi5t4CgtjxuhWUBvQO6_qsULiqUIFckEZty75jYNw5yz6rNqiIKCwm
Clontech的非常好, 感觉. 效果不好可能是RNA问题, 或RTase的问题. 因为目前clontech的RTase是Takara的产品，而非原来clontech的产品，可单购。
