埃替格韦 T2332

Product Introduction
Bioactivity


英文名: Elvitegravir

描述: Elvitegravir (JTK-303) 是一种人类免疫缺陷病毒整合酶链转移抑制剂，作用于 HIV-1IIIB、HIV-2EHO 和 HIV-2ROD，IC50分别为 0.7 nM、2.8 nM 和 1.4 nM。

细胞实验: Elvitegravir (EVG) is prepared in DMSO and stored, and then diluted with appropriate medium before use[1]. MT-2 cells (2×105 cells) are infected with HIV-1 IIIB and then cultured in the presence of 0.5 nM or 0.1 nM Elvitegravir. Cultures are incubated at 37°C until an extensive cytopathic effect (CPE) is observed, and the culture supernatant is then harvested for further passage in fresh MT-2 cells. The concentration of Elvitegravir is increased when a significant CPE is observed. At the indicated passages, proviral DNA is extracted from infected MT-2 cells and then subjected to PCR, followed by direct population-based sequencing. Susceptibility to Elvitegravir at the indicated passages is determined using the MAGI assay or p24 production[1].

体内活性: Elvitegravir抑制MLV感染的复制,IC50为5.8 nM,也抑制灵长类动物的逆转录病毒SIV,IC50为0.5 nM,说明IN抑制剂具有抗多种逆转录病毒的活性。Elvitegravir 抑制整合酶活性,IC50为 6 nM。Elvitegravir 抑制PBMC和PA,IC50 分别为0.89和20 nM。Elvitegravir抑制链转移产物的合成,IC50为54 nM。Elvitegravir通过抑制IN-调节的链转移而抑制整合。EVG具有无血清抗病毒活性,IC50为0.3-0.9 nM,作用于外周血单个核细胞,有效作用于HIV-1和 HIV-2。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 82 mg/mL (183.1 mM)
Ethanol : 33 mg/mL (73.7 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)


关键字: inhibit | HIV-1IIIB | HIV-2EHO | HIV | GS 9137 | JTK 303 | HIV Integrase | cDNA | D-06677 | Inhibitor | GS9137 | HIV-2ROD | JTK303 | Elvitegravir | D 06677 | Human immunodeficiency virus

相关产品: Tripterifordin | Calanolide E | Cabotegravir | Nelfinavir Mesylate | Helichrysetin | Pentosan Polysulfate Sodium (W/W 43%) | Delavirdine mesylate | Obefazimod | Cholic acid sodium | Pepstatin

相关库: FDA-Approved Drug Library | Drug Repurposing Compound Library | Approved Drug Library | FDA-Approved & Pharmacopeia Drug Library | Clinical Compound Library | Bioactive Compounds Library Max | Inhibitor Library | EMA Approved Drug Library | Anti-Viral Compound Library | NO PAINS Compound Library

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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