CAS NO: | 697761-98-1 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
500mg | 电议 |
生物活性 | Elvitegravir (GS-9137; JTK-303; D06677) is anHIV integraseinhibitor forHIV-1IIIB,HIV-2EHOandHIV-2RODwithIC50of 0.7 nM, 2.8 nM and 1.4 nM, respectively. | ||||||||||||||||
IC50& Target | IC50: 0.7 nM (HIV-1IIIB), 2.8 nM (HIV-2EHO), 1.4 nM(HIV-2ROD)[1] | ||||||||||||||||
体外研究 (In Vitro) | Elvitegravir (GS-9137; JTK-303; D06677) blocks the integration of HIV-1 cDNA through the inhibition of DNA strand transfer. Elvitegravir exerts potent anti-HIV activity against not only wild-type strains but also drug-resistant clinical isolates. Interestingly, Elvitegravir also shows antiviral activity against murine leukemia virus (MLV) and simian immunodeficiency virus (SIV). Elvitegravir shows potent antiviral activity against three laboratory strains of HIV, with EC50values in the subnanomolar to nanomolar range. Next, the activity of Elvitegravir is evaluated against wild-type clinical isolates representing various subtypes of HIV-1. Elvitegravir suppresses the replication of all HIV-1 subtypes tested, with an antiviral EC50ranging from 0.1 to 1.26 nM. Moreover, Elvitegravir suppresses the replication of HIV-1 clinical isolates carrying NRTI, NNRTI, and PI resistance-associated genotypes, as did a control IN inhibitor, the compound L-870,810. The cytotoxicities of these inhibitors are also determined using an MTT colorimetric assay. Mean values for the concentration that suppresses the viability of target cells by 50% for Elvitegravir and L-870,810 in PBMC obtained from three independent donors are 4.6±0.5 μM and 2.7±0.6 μM, respectively. Thus, Elvitegravir can suppress various HIV strains, including diverse HIV-1 subtypes and clinical isolates carrying multiple mutations associated with resistance to currently approved antiretroviral drugs[1]. | ||||||||||||||||
Clinical Trial | |||||||||||||||||
分子量 | 447.88 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C23H23ClFNO5 | ||||||||||||||||
CAS 号 | 697761-98-1 | ||||||||||||||||
中文名称 | 埃替格韦 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : 250 mg/mL(558.19 mM;Need ultrasonic) 配制储备液
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以下溶剂前显示的百
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