产品说明书
Elvitegravir
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同义名 : | 埃替格韦 ;GS-9137;JTK-303;brand name: Stribild;EVG;D06677 |
| CAS号 : | 697761-98-1 | |
| 货号 : | A131621 | |
| 分子式 : | C23H23ClFNO5 | |
| 纯度 : | 98% | |
| 分子量 : | 447.884 | |
| MDL号 : | - | |
| 存储条件： |
粉末 Keep in dark place,Inert atmosphere,Room temperature 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 250 mg/mL(558.18 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Human immunodeficiency virus (HIV) encodes three enzymes, reverse transcriptase (RT), protease (PR) and integrase (IN), each of which play important roles in viral replicationElvitegravir: An emerging HIV integrase inhibitor https://www.researchgate.net/publication/244934621_Elvitegravir_An_emerging_HIV_integrase_inhibitor. Elvitegravir (GS-9137) is a HIV-1 integrase strand transfer inhibitor, with IC50 of 0.7 nM, 2.8 nM and 1.4 nM for HIV-1 IIIB, HIV-2 EHO and HIV-2 ROD, respectively[2]. It is also a cytochrome P450 2C9 inducer. Elvitegravir has been developed for treatment of HIV-1 infection. HIV-infected patients were treated with 200 - 800 mg Elvitegravir once daily or 50 mg daily coadministered with ritonavir and it was showed that Elvitegravir achieve Cmax within 3–4 h and the half-life of Elvitegravir was approximately 3 h and was increased to approximately 9 h when coadministered with ritonavir[1]. Elvitegravir suppressed the replication of MLV and primate retrovirus SIV infection with EC50 values of 5.8 nM and 0.5 nM, respectively[2]. Recently, it was found that Elvitegravir inhibits 2019-novel coronavirus in vitro. | ||
| 细胞研究 | |||||
|---|---|---|---|---|---|
| 细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
| human C8166 cells | Function assay | Antiviral activity against HIV1 LAI 3B infected in human C8166 cells assessed as protection against virus-induced cytopathic effect by MTT assay, EC50=0.21 nM | 21763149 | ||
| human MT4 cells | Cytotoxicity assay | Cytotoxicity against human MT4 cells by MTT assay, CC50=1.15 μM | 18665580 | ||
| MT4 cells | Function assay | Antiviral activity against HIV1 3B in MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay, EC50=0.37 nM | 18665580 | ||
| 临床研究 | |||||
|---|---|---|---|---|---|
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT00950859 | Infection, Human Immunodeficie... 展开 >>ncy Virus 收起 << | Phase 2 | Completed | - | - |
| NCT01815736 | - | Active, not recruiting | - | - | |
| NCT00950859 | - | Completed | - | - | |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
|
1 mM 5 mM 10 mM |
2.23mL 0.45mL 0.22mL |
11.16mL 2.23mL 1.12mL |
22.33mL 4.47mL 2.23mL |
