1. GPCR/G Protein Immunology/Inflammation Anti-infection
  2. CXCR HIV
  3. Plerixafor

Plerixafor  (Synonyms: 普乐沙福; AMD 3100; JM3100; SID791)

目录号: HY-10046 纯度: 99.90%
COA 产品使用指南

Plerixafor (AMD 3100) 是选择性的 CXCR4 拮抗剂,IC50 为 44 nM。Plerixafor 是一种免疫刺激剂和造血干细胞动员剂,也是 CXCR7 的变构激动剂。Plerixafor 抑制 HIV-1HIV-2 的复制,EC50 为 1-10 nM。

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Plerixafor Chemical Structure

Plerixafor Chemical Structure

CAS No. : 110078-46-1

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Customer Review

Other Forms of Plerixafor:

MCE 顾客使用本产品发表的 66 篇科研文献

RT-PCR
WB
IF
Proliferation Assay
IHC

    Plerixafor purchased from MCE. Usage Cited in: Cancer Lett. 2022 Oct 7;551:215944.  [Abstract]

    Viability of cells treated with combinations different concentrations of AMD3100 and Olaparib for 24 h.

    Plerixafor purchased from MCE. Usage Cited in: Cancer Lett. 2022 Oct 7;551:215944.  [Abstract]

    Immunohistochemical staining of proliferation-related protein, Ki-67, in breast cancer after treatment with control, AMD3100 (2.5 mg/kg), Olaparib, or a combination of AMD3100 and Olaparib.

    Plerixafor purchased from MCE. Usage Cited in: Cell Death Dis. 2022 Feb 4;13(2):118.  [Abstract]

    PGK1 induced the CXCR4-mediated phosphorylation of AKT (p-AKT) and ERK (p-ERK), and blockade of CXCR4 signaling by AMD3100 (48 h) treatment did not alter cellular PGK1 expression in KIRC cells.

    Plerixafor purchased from MCE. Usage Cited in: Bioact Mater. 2021 Jan 7;6(7):2039-2057.  [Abstract]

    Western blot analysis of the expression of CXCR4, integrin αvβ3, p-Jak2, Jak2, p-FAK, FAK, p-STAT3 and STAT3 in MSCs (pretreated with a CXCR4 inhibitor (AMD3100; 20 μM; pretreated with 1 h) and an integrin αvβ3 inhibitor (cyclo(-RGDfK))) after the addition of 152RM for 24 h.

    Plerixafor purchased from MCE. Usage Cited in: Theranostics. 2021 Jan 1;11(6):2612-2633.  [Abstract]

    Transwell assays indicated that AMD3100 treatment (1 µg/ml, 24 hours) significantly decreases the migration and invasion of Caco-2-HOXB5 cells.

    Plerixafor purchased from MCE. Usage Cited in: Theranostics. 2021 Jan 1;11(6):2612-2633.  [Abstract]

    Caco-2 cells are incubated with vehicle or AMD3100 (1 µg/ml, 24 hours) after lentivirus transfection (LV-HOXB5), then Western blotting assays are conducted to measure the protein levels of CXCL12, HOXB5, CXCR4, p-ERK and p-ETS1 in the indicated cell lines.

    Plerixafor purchased from MCE. Usage Cited in: Adv Funct Mater. 2020, 2000309.

    NOD/SCID mice were i.p. injected with AMD3100 (4 mg/kg). After 1 h, the mice are i.v. injected with iFluor 647-labeled Aazo@CMSN. At 12 h after nanoparticle injection, the mouse craniums are excised for the observation of nanoparticle bone marrow niches targeting under CLSM. Pre-treatment with AMD3100 significantly declined the bone marrow niches targeting of the nanoparticles.

    Plerixafor purchased from MCE. Usage Cited in: Cell Mol Immunol. 2020 Mar;17(3):283-299.  [Abstract]

    ELISA of IL-1β in supernatants of BV2 cells stimulated with gp120 LAV (0.5 μg/mL) for 24 h in the presence of increasing doses of a CXCR4-specific inhibitor (AMD3100, 0.1-10 μM; prestimulated with 30 min-2 h).

    Plerixafor purchased from MCE. Usage Cited in: Oncogene. 2019 Jun;38(25):5021-5037.  [Abstract]

    IF staining of the tumor tissue sections showed decreased Ki67 and a reversal of EMT markers indicated by increased E-cadherin and decreased N-cadherin expression in the AMD3100 (5 mg/kg or 3.5 mg/kg) treated groups.

    Plerixafor purchased from MCE. Usage Cited in: Oncogene. 2019 Jun;38(25):5021-5037.  [Abstract]

    Additional EMT-related proteins (Snail and Slug) are downregulated by AMD3100 (5 mg/kg or 3.5 mg/kg) in tumor samples from both diet groups, as quantified by immunoblotting.

    Plerixafor purchased from MCE. Usage Cited in: Cell Physiol Biochem. 2018;46(3):890-906.  [Abstract]

    The protein expression of LRRC4, SDF-1, CXCR4, ERK, Slit2 and VEGF in the brain tissue of rats is determined by Western blotting.

    Plerixafor purchased from MCE. Usage Cited in: Int J Biol Sci. 2017 May 5;13(5):604-614.  [Abstract]

    Epithelial cells with or without AMD3100 pretreatment are cultured in conditioned medium (CM) from LPS-treated NFs or LTA-treated NFs for 3 days, and the secretion of TNF-α in the supernatant of culture is detected by ELISA. Epithelial cells cultured in MSM are used as control. Both LPS-treated NFs and LTA-treated NFs enhanced the section of TNF-α by epithelial cells compared with control. Pretreatment of epithelial cells with AMD3100 significantly attenuates the increase of TNF-α.

    查看 CXCR 亚型特异性产品:

    查看 HIV 亚型特异性产品:

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Plerixafor (AMD 3100) is a selective CXCR4 antagonist with an IC50 of 44 nM. Plerixafor, an immunostimulant and a hematopoietic stem cell (HSC) mobilizer, is an allosteric agonist of CXCR7. Plerixafor inhibits HIV-1 and HIV-2 replication with an EC50 of 1-10 nM[1][2][3][4][7].

    IC50 & Target[3][7]

    125I-CXCL12-CXCR4

    44 nM (IC50)

    125I-CXCL12-CXCR7

     

    HIV-1

    1-10 nM (EC50)

    HIV-2

    1-10 nM (EC50)

    体外研究
    (In Vitro)

    CXCR4 抑制剂 Plerixafor (AMD3100) 是一种有效的 CXCL12 介导的趋化性抑制剂 (IC50,5.7 nM),效力略优于其对 CXCR4 的亲和力。Plerixafor 干扰 CXCR4 与其天然配体 SDF-1 (CXCL12) 的相互作用。用 CCX771 或 CXCL11 处理细胞对 CXCL12 介导的 MOLT-4 或 U937 TEM 没有影响。相反,10 μM Plerixafor 在两种细胞系中抑制 CXCL12 介导的 TEM[1]
    Plerixafor 可防止肿瘤相关巨噬细胞 (TAM) 浸润到肿瘤组织中[8]

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

    体内研究
    (In Vivo)

    Plerixafor (2 mg/kg) 对 UUO 小鼠给药会加剧肾间质 T 细胞浸润,导致促炎细胞因子 IL-6IFN-γ 的产生增加,并降低抗炎细胞因子 IL-10 的表达[5]
    CXCR4 拮抗剂 Plerixafor (AMD3100) 在 8 周时显著减少了血管周围和间质纤维化[6]。LD50,小鼠,SC:16.3 mg/kg;LD50,大鼠,SC:>50 mg/kg;LD50,小鼠和大鼠,静脉注射:5.2 mg/kg[5]

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

    Clinical Trial
    分子量

    502.78

    Formula

    C28H54N8

    CAS 号
    性状

    固体

    颜色

    White to off-white

    中文名称

    普乐沙福

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    溶解性数据
    细胞实验: 

    Ethanol 中的溶解度 : 50 mg/mL (99.45 mM; 超声助溶)

    DMSO 中的溶解度 : 1.92 mg/mL (3.82 mM; ultrasonic and warming and adjust pH to 7 with 1 M HCL and heat to 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)

    H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 1.9889 mL 9.9447 mL 19.8894 mL
    5 mM 0.3978 mL 1.9889 mL 3.9779 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。-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。

    • 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% EtOH    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 3 mg/mL (5.97 mM); 澄清溶液

      此方案可获得 ≥ 3 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 30.0 mg/mL 的澄清 EtOH 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% EtOH    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 3 mg/mL (5.97 mM); 澄清溶液

      此方案可获得 ≥ 3 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 30.0 mg/mL 的澄清 EtOH 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

      20% SBE-β-CD in Saline 的配制(4°C,储存一周):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。
    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

    由于实验过程有损耗,建议您多配一只动物的量
    请输入您的动物体内配方组成:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
    您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
    连续给药周期超过半月以上,请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
    纯度 & 产品资料

    纯度: 99.90%

    参考文献
    Cell Assay
    [2]

    U87MG cells are seeded in 96-well plates at the density of 6×103 cells in 200 μL/well and treated with CXCL12, Plerixafor or with peptide R. MTT (5 μg/mL) is added at each time point (24, 48, 72 h) during the final 2 h of treatment. After removing cell medium, 100 μL DMSO are added and optical densities measured at 595 nm with a LT-4000MS Microplate Reader. Measurements are made in triplicates from three independent experiments[2].

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

    Animal Administration
    [3][4]

    Mice[3]
    Male C57bl/6 mice (6-7 weeks old, weighing 20 g) are used. The animals are acclimated to the housing environment, which is SPF and had a temperature of 22°C and a 12h/12h light/dark cycle for a week. Then, they are randomly divided into following experimental groups, with 8 mice in each group: normal (no specific intervention), UUO+AMD3100 (mice received UUO surgery and 2 mg/kg AMD3100), and UUO+PBS (mice received UUO surgery and the same volume of PBS). AMD3100 and PBS are administered via intraperitoneal injection every day until sacrifice.
    Rats[4]
    The CXCR4 antagonist, AMD3100 dissolved in H2O, is delivered in the type 2 diabetic sand rat model at a dose of 6 mg/kg per day for 8 weeks. In complementary studies, the effect of CXCR4 antagonism (AMD3100 6mg/kg/d) on regulatory T cell numbers is examined. For these studies, AMD3100 or vehicle is delivered via minipump for a period of one week.

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

    参考文献

    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。-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 / Ethanol 1 mM 1.9889 mL 9.9447 mL 19.8894 mL 49.7235 mL
    Ethanol 5 mM 0.3978 mL 1.9889 mL 3.9779 mL 9.9447 mL
    10 mM 0.1989 mL 0.9945 mL 1.9889 mL 4.9724 mL
    15 mM 0.1326 mL 0.6630 mL 1.3260 mL 3.3149 mL
    20 mM 0.0994 mL 0.4972 mL 0.9945 mL 2.4862 mL
    25 mM 0.0796 mL 0.3978 mL 0.7956 mL 1.9889 mL
    30 mM 0.0663 mL 0.3315 mL 0.6630 mL 1.6575 mL
    40 mM 0.0497 mL 0.2486 mL 0.4972 mL 1.2431 mL
    50 mM 0.0398 mL 0.1989 mL 0.3978 mL 0.9945 mL
    60 mM 0.0331 mL 0.1657 mL 0.3315 mL 0.8287 mL
    80 mM 0.0249 mL 0.1243 mL 0.2486 mL 0.6215 mL
    Help & FAQs
    • 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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    产品名称:
    Plerixafor
    目录号:
    HY-10046
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