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Elvitegravir

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Chemical Structure| 697761-98-1 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 : MFCD11846135
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

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

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