2. Metabolic Enzyme/Protease Anti-infection
  3. HIV Integrase HIV
  4. Raltegravir potassium

Raltegravir potassium  (Synonyms: 雷特格韦钾盐; MK 0518 potassium)

目录号: HY-10353A 纯度: 99.82%
Data Sheet SDS COA 产品使用指南 技术支持

溶解度

动物溶解方案

实验小贴士

Raltegravir (MK 0518) potassium 是一种有效的 integrase 抑制剂，用于研究 HIV 感染。

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Raltegravir potassium Chemical Structure

Raltegravir potassium Chemical Structure

CAS No. : 871038-72-1

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥320
In-stock
5 mg ￥300
In-stock
10 mg ￥450
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50 mg ￥1300
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100 mg ￥2200
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500 mg   询价  

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Customer Review

Other Forms of Raltegravir potassium:

Raltegravir potassium 相关抗体

Top Publications Citing Use of Products

    Raltegravir potassium 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 potassium 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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    HIV HIV-1 HIV-2

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Raltegravir (MK 0518) potassium is a potent integrase (IN) inhibitor, used to treat HIV infection.

    细胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    HEK-293T IC50
    2 nM
    Compound: 1, RAL, Raltegravir
    Antiviral activity against pseudo Human immunodeficiency virus infected in HEK293T cells after 2 days
    Antiviral activity against pseudo Human immunodeficiency virus infected in HEK293T cells after 2 days
    		[PMID: 23845180]
    HEK-293T IC50
    7.1 nM
    Compound: 1, RAL, Raltegravir
    Antiviral activity against pseudo Human immunodeficiency virus infected in HEK293T cells after 2 days in presence of human serum albumin
    Antiviral activity against pseudo Human immunodeficiency virus infected in HEK293T cells after 2 days in presence of human serum albumin
    		[PMID: 23845180]
    MT2 EC50
    0.26 nM
    Compound: RAL, Raltegravir, MK-0518
    Antiviral activity against Human immunodeficiency virus 1 3B infected in human MT2 cells assessed as inhibition of virus induced cytopathic effect measured after 2 to 3 days by PCR
    Antiviral activity against Human immunodeficiency virus 1 3B infected in human MT2 cells assessed as inhibition of virus induced cytopathic effect measured after 2 to 3 days by PCR
    		[PMID: 21115794]
    MT2 EC50
    0.26 nM
    Compound: RAL, Raltegravir, MK-0518
    Antiviral activity against Human immunodeficiency virus 1 3B harboring integrase T124A mutant gene infected in human MT2 cells assessed as inhibition of virus induced cytopathic effect selected after 14 passages measured after 2 to 3 days by PCR
    Antiviral activity against Human immunodeficiency virus 1 3B harboring integrase T124A mutant gene infected in human MT2 cells assessed as inhibition of virus induced cytopathic effect selected after 14 passages measured after 2 to 3 days by PCR
    		[PMID: 21115794]
    MT2 EC50
    0.26 nM
    Compound: RAL, Raltegravir, MK-0518
    Antiviral activity against Human immunodeficiency virus 1 3B harboring integrase T124A,Q148K,N155H/I204T mutant infected in human MT2 cells assessed as inhibition of virus-induced effect selected on day 28 after 8 passages by PCR
    Antiviral activity against Human immunodeficiency virus 1 3B harboring integrase T124A,Q148K,N155H/I204T mutant infected in human MT2 cells assessed as inhibition of virus-induced effect selected on day 28 after 8 passages by PCR
    		[PMID: 21115794]
    MT2 EC50
    1.3 nM
    Compound: RAL, Raltegravir, MK-0518
    Antiviral activity against Human immunodeficiency virus 1 3B harboring integrase G59E, T124A,Q148K, Q148R,N155H, N155H/I204T mutant infected in human MT2 cells assessed as inhibition of virus-induced effect selected on day 42 after 12 passages by PCR
    Antiviral activity against Human immunodeficiency virus 1 3B harboring integrase G59E, T124A,Q148K, Q148R,N155H, N155H/I204T mutant infected in human MT2 cells assessed as inhibition of virus-induced effect selected on day 42 after 12 passages by PCR
    		[PMID: 21115794]
    MT2 EC50
    32 nM
    Compound: RAL, Raltegravir, MK-0518
    Antiviral activity against Human immunodeficiency virus 1 3B harboring integrase T124A,Q148K,Q148R,E138K/Q148K,E138K/Q148R,G140S/Q148R,V151I/N155H,N155H/I204T,N17S/Q148K/G163R,T124A/V151I/N155H,E138K/Q148K/G163R,G140C/Q148K/G163R,E92Q/E138K/Q148K/M154I mu
    Antiviral activity against Human immunodeficiency virus 1 3B harboring integrase T124A,Q148K,Q148R,E138K/Q148K,E138K/Q148R,G140S/Q148R,V151I/N155H,N155H/I204T,N17S/Q148K/G163R,T124A/V151I/N155H,E138K/Q148K/G163R,G140C/Q148K/G163R,E92Q/E138K/Q148K/M154I mu
    		[PMID: 21115794]
    MT2 EC50
    6.4 nM
    Compound: RAL, Raltegravir, MK-0518
    Antiviral activity against Human immunodeficiency virus 1 3B harboring integrase T124A,Q148K,Q148R,N17S/Q148K,E92Q/M154I,G140C/Q148K,G140S/Q148R,Q148K/G163R,V151I/N155H, N155H/I204T,T124A/V151I/N155H,G140C/Q148K/G163R mutant infected in human MT2 cells as
    Antiviral activity against Human immunodeficiency virus 1 3B harboring integrase T124A,Q148K,Q148R,N17S/Q148K,E92Q/M154I,G140C/Q148K,G140S/Q148R,Q148K/G163R,V151I/N155H, N155H/I204T,T124A/V151I/N155H,G140C/Q148K/G163R mutant infected in human MT2 cells as
    		[PMID: 21115794]
    MT2 EC50
    6.4 nM
    Compound: RAL, Raltegravir, MK-0518
    Antiviral activity against Human immunodeficiency virus 1 3B harboring integrase T124A, Q148K,Q148R, N155H, E92Q/M154I,Q148K/G163R, N155H/I204T mutant infected in human MT2 cells assessed as inhibition of virus-induced effect selected on day 56 after 16 p
    Antiviral activity against Human immunodeficiency virus 1 3B harboring integrase T124A, Q148K,Q148R, N155H, E92Q/M154I,Q148K/G163R, N155H/I204T mutant infected in human MT2 cells assessed as inhibition of virus-induced effect selected on day 56 after 16 p
    		[PMID: 21115794]
    MT4 CC50
    > 51.8 μM
    Compound: Raltegravir-K
    Cytotoxic activity against mock-infected human MT4 cellls assessed as reduction in cell viability by MTT assay
    Cytotoxic activity against mock-infected human MT4 cellls assessed as reduction in cell viability by MTT assay
    		[PMID: 28951095]
    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 IC95 of 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.

    Raltegravir potassium 相关抗体:
    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
    NCT NumberSponsorConditionStart DatePhase
    NCT00809718The University of Texas Health Science Center at San Antonio|Merck Sharp & Dohme LLC|Centers for Disease Control and Prevention|VA Office of Research and Development
    Healthy
    		February 2009Phase 1
    NCT00870363University of California, Davis
    HIV Infections
    		April 2009Phase 4
    NCT01114425Groupe d´Etude sur le Risque d´Exposition des Soignants aux Agents Infectieux|Merck Sharp & Dohme LLC
    HIV Infections
    		November 1, 2010Phase 3
    分子量

    482.51

    Formula

    C20H20FKN6O5
    CAS 号
    性状

    固体

    颜色

    White to off-white

    中文名称

    雷特格韦钾盐；拉替拉韦钾盐
    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    溶解性数据
    细胞实验： 

    H2O 中的溶解度 : 25 mg/mL (51.81 mM; 超声助溶)

    DMSO 中的溶解度 : 20.83 mg/mL (43.17 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.0725 mL 10.3625 mL 20.7250 mL
    5 mM 0.4145 mL 2.0725 mL 4.1450 mL
    查看完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
    储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时，请在6个月内使用， -20°C储存时，请在1个月内使用。

    * 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    动物实验：

    请根据您的 实验动物和给药方式 选择适当的溶解方案。

    以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
    ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
    以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

    • 方案 一

      请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL (4.31 mM); 澄清溶液

      此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

      生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
    • 方案 二

      请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.08 mg/mL (4.31 mM); 澄清溶液

      此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。

      2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。

    以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比； 如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。

    • 方案 一

      请依序添加每种溶剂： PBS

      Solubility: 25 mg/mL (51.81 mM); 澄清溶液; 超声助溶

    扫码获得
    动物溶解方案

    动物溶解方案计算器
    请输入动物实验的基本信息：

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    只
    由于实验过程有损耗，建议您多配一只动物的量
    纯度 & 产品资料

    纯度： 99.96%

    Data Sheet (626 KB) SDS (393 KB)

    COA (286 KB)HNMR (189 KB)LCMS (338 KB)

    产品使用指南 (1538 KB)
    参考文献
    Cell Assay
    [5]

    Human MT-4 cells are infected for 2 hours with the SIVmac251, HIV-1 (IIIB) and HIV-2 (CDC 77618) stocks at a multiplicity of infection of, approximately, 0.1. Cells are then washed three times in phosphate buffered saline, and suspended at 5 × 105/mL in fresh culture medium (to primary cells 50 units/mL of IL-2 are added) in 96-well plates, in the presence or absence of a range of triplicate raltegravir concentrations (0.0001 μM-1 μM). Untreated infected and mock-infected controls are prepared too, in order to allow comparison of the data derived from the different treatments. Viral cytopathogeniciy in MT-4 cells is quantitated by the methyl tetrazolium (MTT) method (MT-4/MTT assay) when extensive cell death in control virus-infected cell cultures is detectable microscopically as lack of capacity to re-cluster. The capability of MT-4 cells to form clusters after infection. Briefly, clusters are disrupted by pipetting; and, after 2 hours of incubation at 37°C, the formation of new clusters is assessed by light microscopy (100× magnification). Cell culture supernatants are collected for HIV-1 p24 and HIV-2/SIVmac251 p27 core antigen measurement by ELISA. In CEMx174-infected cell cultures, which show a propensity to form syncytia induced by the virus envelope glycoproteins, syncytia are counted, in blinded fashion, by light microscopy for each well at 5 days following infection.

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

    Raltegravir potassium 相关分类

    完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
    储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时，请在6个月内使用， -20°C储存时，请在1个月内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO / H2O 1 mM 2.0725 mL 10.3625 mL 20.7250 mL 51.8124 mL
    5 mM 0.4145 mL 2.0725 mL 4.1450 mL 10.3625 mL
    10 mM 0.2072 mL 1.0362 mL 2.0725 mL 5.1812 mL
    15 mM 0.1382 mL 0.6908 mL 1.3817 mL 3.4542 mL
    20 mM 0.1036 mL 0.5181 mL 1.0362 mL 2.5906 mL
    25 mM 0.0829 mL 0.4145 mL 0.8290 mL 2.0725 mL
    30 mM 0.0691 mL 0.3454 mL 0.6908 mL 1.7271 mL
    40 mM 0.0518 mL 0.2591 mL 0.5181 mL 1.2953 mL
    H2O 50 mM 0.0414 mL 0.2072 mL 0.4145 mL 1.0362 mL

    * 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

    Help & FAQs
    • 抗体抑制剂请问怎么灭菌呢？

      我们的抗体抑制剂产品本身就是无菌的，细胞实验可以用培养基稀释，动物实验可以用无菌 PBS 或者生理盐水稀释。

    • 抗体抑制剂的人源化，人鼠嵌合抗体有什么区别呢？

      人鼠嵌合抗体由鼠源可变区+人源恒定区组成，人源化约65%，免疫原性较高。人源化抗体仅保留鼠源CDR，其余为人源结构，人源化约90%，免疫原性较低。相比嵌合抗体，人源化抗体更接近人体抗体，安全性更高。

    Keywords:

    Raltegravir871038-72-1MK 0518雷特格韦钾盐拉替拉韦钾盐MK0518MK-0518HIV IntegraseHIVHuman immunodeficiency virusInhibitorinhibitorinhibit

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