产品属性:
产品名称 | 规格 | CAS号 | 型号 |
HIV-1 integrase inhibitor | 5mg 10mg 50mg 200mg | 544467-07-4 | EY-Y0164716 |
Cas No.544467-07-4
别名
化学名 (Z)-4-[3-(azidomethyl)phenyl]-4-hydroxy-2-oxobut-3-enoic acid
分子式 C11H9N3O4
![HIV-1 integrase inhibitor.png HIV-1 integrase inhibitor.png](/SupplyImg/2022-11-28/6380523172649664578452243.jpg)
分子量 247.21
溶解度 Soluble in DMSO
储存条件 Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述:
HIV-1 integrase inhibitor is useful for anti-HIV, with IC50 value of 0.33 μM,[1] which can target HIV-1 integrase and depress the activity in the treatment of HIV infection, AIDS, and other similar diseases characterized by integration of a retroviral genome into a host chromosome.
HIV integrase is a 32 kDa protein produced from the C-terminal portion of the Pol gene product, an enzyme produced by HIV that enables its genetic material to be integrated into the DNA of the infected cell [2]which are not to be confused with phage integrases and a key component in the retroviral pre-integration complex (PIC)[3]. HIV-1 integrase is composed of 3 structurally independent, functional domains: the N-terminal domain (NTD), catalytic core domain (CCD) and the C-terminal domain (CTD).The HIV-1 integration occurs through a multistep process that includes two catalytic reactions: 3'endonucleolytic processing of proviral DNA ends (termed 3'processing) and integration of 3'-processed viral DNA into cellular DNA (referred to as strand transfer)[4].
The human immunodeficiency virus (HIV) is the causative agent for the acquired immunodeficiency syndrome (AIDS)[5], then HIV integrase is an attractive target for new anti-HIV drugs. The drug design of HIV-1 integrase inhibitor include integrase strand transfer inhibitors (INSTIs),inhibition of the LEDGF/p75- integrase interaction and integrase binding inhibitors, but strand transfer inhibition is the most intuitively obvious and readily pursued to date.Mg2+ and Mn2+ are critical cofactors in the integration phase, so removing these cofactors (e.g. through chelation) causes functional impairment of integrase[6].Competitive inhibitors compete directly with viral DNA for binding to integrase in order to inhibit 3‘-end processing.[7] In doing this the inhibitors completely block the active site from binding to target DNA.INSTIs bind tightly and specifically to the IN that is associated with the ends of the DNA by chelating the divalent metal ions (Mg2+) which is coordinated by the catalytic triad, such as the DDE motif which is located in the CCD and is the active site of the enzyme[8].
Development of a successful INSTI treatment was accomplished when raltegravir was discovered by Merck Sharp & Dohme Limited.[9] S/GSK1349572 is an integrase inhibitor discovered by ViiV/Shinongi which was entering phase three in clinical trials in 2011. This new drug is promising and seems to be well tolerated and so far shows better results than both raltegravir and elvitegravir.[10]
关键字: 544467-07-4;C11H9N3O4;HIV-1 integrase inhi;
上海一研生物科技有限公司Shanghai yiyan bio-technology Co. Ltd.主要从事免疫学、分子生物学和常规生化试剂等为一体的科研产品销售企业,公司自成立以来,秉承""全心全意服务于科研工作者""的企业理念,立足生物科技领域,运用生物技术和科研试剂,发展现代生物科技,为各类大中小医院及其它医疗机构、高等院校、科研院所、企事业单位提供优质的产品,服务生物科技领域的科学研究人员。
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