1. Metabolic Enzyme/Protease Anti-infection
  2. HIV Integrase HIV
  3. Raltegravir sodium

Raltegravir sodium  (Synonyms: MK 0518 sodium)

目录号: HY-10353B
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Raltegravir (MK 0518) sodium 是一种有效的、具有口服活性的 HIV 整合酶(IN)抑制剂。

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Raltegravir sodium Chemical Structure

Raltegravir sodium Chemical Structure

CAS No. : 1292804-07-9

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Raltegravir sodium 的其他形式现货产品:

Customer Review

Other Forms of Raltegravir sodium:

    Raltegravir sodium purchased from MCE. Usage Cited in: J Neuroimmune Pharmacol. 2017 Dec;12(4):682-692.  [Abstract]

    TDF/FTC/RAL combined medication induces mouse NPC apoptosis in vitro. Mouse NPCs are treated with either DMSO or TDF/FTC/RAL for 8 h. Cleaved Caspase-3 levels are determined by Western blotting.

    Raltegravir sodium purchased from MCE. Usage Cited in: J Virol. 2017 Jan 18;91(3). pii: e02152-16.  [Abstract]

    Inhibitory effects of Raltegravir on pUL89-C activity analyzed by agarose gel assay. Linearized pUC18 in the absence (Lane 1) or presence (Lane 2) of pUL89-C. Lanes 3–10: A range of concentrations of Raltegravir with pUL89-C. Numbers above bands correspond to the fold change compared with the control.

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    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Raltegravir (MK 0518) sodium is a potent and orally active integrase (IN) inhibitor, used to treat HIV infection.

    体外研究
    (In Vitro)

    PFV IN carrying the S217H substitution is 10-fold less susceptible to Raltegravir with IC50 of 900 nM. PFV IN displays 10% of WT activity and is inhibited by Raltegravir with an IC50 of 200 nM, indicating a appr twofold decrease in susceptibility to the IN strand transfer inhibitor (INSTI) compared with WT IN. S217Q PFV IN is as sensitive to Raltegravir as the WT enzyme[1]. Raltegravir is metabolized by glucuronidation, not hepatically. Raltegravir has potent in vitro activity against HIV-1, with a 95% inhibitory concentration of 31±20 nM, in human T lymphoid cell cultures. Raltegravir is also active against HIV-2 when Raltegravir is tested in CEMx174 cells, with an IC95of 6 nM. Raltegravir metabolism occurs primarily through glucuronidation. Drugs that are strong inducers of the glucuronidation enzyme, UGT1A1, significantly reduce Raltegravir concentrations and should not be used. Raltegravir exhibits weak inhibitory effects on hepatic cytochrome P450 activity. Raltegravir does not induce CYP3A4 RNA expression or CYP3A4-dependent testosterone 6-β-hydroxylase activity[2]. Raltegravir cellular permeativity is reduced in the presence of magnesium and calcium[3]. Raltegravir and related HIV-1 integrase (IN) strand transfer inhibitors (INSTIs efficiently block viral replication[4]. In acutely infected human lymphoid CD4+ T-cell lines MT-4 and CEMx174, SIVmac251 replication is efficiently inhibited by Raltegravir, which shows an EC90 in the low nanomolar range[5].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    体内研究
    (In Vivo)

    Raltegravir induces viro-immunological improvement of nonhuman primates with progressing SIVmac251 infection. One non-human primate shows an undetectable viral load following Raltegravir monotherapy[5].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Clinical Trial
    分子量

    466.40

    Formula

    C20H20FN6NaO5

    CAS 号
    中文名称

    雷特格韦钠盐;拉替拉韦钠盐

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式

    Please store the product under the recommended conditions in the Certificate of Analysis.

    纯度 & 产品资料
    参考文献

    Raltegravir sodium 相关分类

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    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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