
簡要描述:Dolutegravir sodium(GSK1349572) 1051375-19-9Dolutegravir sodium salt(DTG; GSK1349572) is a HIV integrase inhibitor(IC50= 2.7 nM),
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| 品牌 | absin | CAS | 1051375-19-9 |
|---|---|---|---|
| 分子式 | C20H18F2N3NaO5 | 純度 | 98% |
| 分子量 | 441.36 | 貨號 | abs47027998 |
| 規(guī)格 | 2mg | 供貨周期 | 現(xiàn)貨 |
| 主要用途 | is a HIV integrase inhibitor | 應(yīng)用領(lǐng)域 | 化工,生物產(chǎn)業(yè),農(nóng)林牧漁,制藥/生物制藥,綜合 |
Dolutegravir sodium(GSK1349572) 1051375-19-9
| 產(chǎn)品描述 | |
| 描述 | Dolutegravir sodium salt(DTG; GSK1349572) is a HIV integrase inhibitor(IC50= 2.7 nM), modest activity against raltegravir-resistant signature mutants Y143R, Q148K, N155H, and G140S/Q148H. |
| 純度 | 98% |
| 儲存/保存方法 | Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution. |
| 基本信息 | |
| 可溶性/溶解性 | 200 mM in DMSO |
| 生物活性 | |
| 靶點 | HIV integrase |
| In vitro(體外研究) | Dolutegravir(S/GSK1349572) inhibits HIV-1 integrase-catalyzed strand transfer with a 50% inhibitory concentration (IC50) of 2.7 nM. S/GSK1349572 inhibits both the HIV integration reaction strand transfer step in vitro and HIV replication in cells with similar potencies. The inhibitor has no effect on total viral DNA synthesis in infected cells but blocks the integration of viral DNA into host DNA with the same potency as its antiviral effect. |
| In vivo(體內(nèi)研究) | The bioavailability of dolutegravir was high when administered as a solution, but was limited by dissolution rate or solubility when administered as a suspension. Dolutegravir is the major circulating component in mice, rats, and monkeys, with direct ether glucuronidation shown to be the primary biotransformation pathway. Dolutegravir is primarily eliminated via the feces either unabsorbed or by hydrolysis of the glucuronide or glucose conjugate. |
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| 研究領(lǐng)域 | |
| 研究領(lǐng)域 | Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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