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Elvitegravir/埃替拉韦 {[allProObj[0].p_purity_real_show]}

货号:A131621 同义名: 埃替格韦 / GS-9137; JTK-303

Elvitegravir是一种 HIV 整合酶抑制剂,主要用于治疗 HIV 感染,其 IC50 对 HIV-1 和 HIV-2 分别为 0.7 nM 和 2.8 nM。

Elvitegravir/埃替拉韦 化学结构 CAS号:697761-98-1
Elvitegravir/埃替拉韦 化学结构
CAS号:697761-98-1
Elvitegravir/埃替拉韦 3D分子结构
CAS号:697761-98-1
Elvitegravir/埃替拉韦 化学结构 CAS号:697761-98-1
Elvitegravir/埃替拉韦 3D分子结构 CAS号:697761-98-1
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Elvitegravir/埃替拉韦 纯度/质量文件 产品仅供科研

货号:A131621 标准纯度: {[allProObj[0].p_purity_real_show]}
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Elvitegravir/埃替拉韦 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.

Elvitegravir/埃替拉韦 细胞研究

细胞系 浓度 检测类型 检测时间 活性说明 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

Elvitegravir/埃替拉韦 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 - -

Elvitegravir/埃替拉韦 实验方案

计算器
存储液制备 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

Elvitegravir/埃替拉韦 技术信息

CAS号697761-98-1
分子式C23H23ClFNO5
分子量 447.88
SMILES Code O=C(C1=CN([C@@H](C(C)C)CO)C2=C(C=C(CC3=CC=CC(Cl)=C3F)C(OC)=C2)C1=O)O
别名 埃替格韦 ;GS-9137; JTK-303; Stribild; EVG; D06677
运输蓝冰
InChI Key JUZYLCPPVHEVSV-LJQANCHMSA-N
Pubchem ID 5277135
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry,2-8°C

溶解方案

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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