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Dolutegravir (GSK1349572)
| 品牌 | 厂商性质 | 产地 | 货期 |
|---|---|---|---|
| 阿拉丁 | 生产商 | 上海 | 现货 |
| 货号 | CAS号 | 操作 |
|---|---|---|
| D127636-50mg | 1051375-16-6 | 询价 |
| D127636-5mg | 1051375-16-6 | 询价 |
| D127636-10mg | 1051375-16-6 | 询价 |
- 分子式 C20H19F2N3O5
- 分子量419.38
属性
| 溶解性 | Soluble in DMSO (84 mg/ml at 25 °C), water (<1 mg/ml at 25 °C), and ethanol (<1 mg/ml at 25 °C). |
| 存贮条件 | 储存温度-20°C |
描述
| 应用 | Dolutegravir (GSK1349572)是一种HIV整合酶抑制剂，IC50为2.7 nM，适度有效作用于抗Raltegravir的显著突变体Y143R， Q148K， N155H，和G140S/Q148H。 |
| 产品介绍 | S/GSK1349572 inhibits recombinant HIV-1 integrase-catalyzed strand transfer in vitro. S/GSK1349572 potently inhibits HIV replication in cells infected with a self-inactivating PHIV lentiviral vector, such as peripheral blood mononuclear cells (PBMCs), MT-4 cells and CIP4. S/GSK1349572 exhibits potent activity against five different nonnucleoside reverse transcription inhibitor--resistant or nucleoside reverse transcription inhibitor--resistant viruses in vitro. S/GSK1349572 shows equivalent activity against two protease inhibitor-resistant viruses similarly to that against wild-type virus. |
| 备注 | S/GSK1349572 (GSK1349572) is a two-metal-binding HIV integrase inhibitor with IC50 of 2.7 nM, modest activity against raltegravir-resistant signature mutants Y143R, Q148K, N155H, and G140S/Q148H. Phase 3. |
| 生化机理 |
Dolutegravir (DTG, GSK1349572) is an integrase inhibitor being developed for the treatment of human immunodeficiency virus (HIV)-1 infection by GlaxoSmithKline (GSK) on behalf of Shionogi-ViiV Healthcare LLC. Dolutegravir (DTG, GSK1349572) is metabolized primarily by uridine diphosphate glucuronyltransferase (UGT)1A1, with a minor role of cytochrome P450 (CYP)3A, and with renal elimination of unchanged drug being extremely low (< 1% of the dose). Fifty-three percent of the total oral dose is excreted unchanged in the feces but it is unknown if all or part of this is due to unabsorbed drug or some percentage of biliary excretion of the glucuronide conjugate which can be further degraded to form the parent compound in the gut lumen. The current Food and Drug Administration (FDA) draft guidance for renal impairment studies states that a pharmacokinetic (PK) study in patients with renal impairment should be conducted even for those drugs primarily metabolized or secrete |
| 别名 | (4R,12AS)-N-[(2,4-二氟苯基)甲基]-3,4,6,8,12,12A-六氢-7-羟基-4-甲基-6,8-二氧代-2H-吡啶并[1',2':4,5]吡嗪并[2,1-B][1,3]嗪-9-甲酰胺;Dolutegravir;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)- |
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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途