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

Plerixafor octahydrochloride  (Synonyms: 鹽酸普樂沙福; AMD3100 octahydrochloride; JM3100 octahydrochloride; SID791 octahydrochloride)

目錄號: HY-50912 純度: 99.09%
COA 產品使用指南

Plerixafor octahydrochloride (AMD3100 octahydrochloride) 是一種選擇性的 CXCR4 拮抗劑, IC50 為 44 nM。

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Plerixafor octahydrochloride Chemical Structure

Plerixafor octahydrochloride Chemical Structure

CAS No. : 155148-31-5

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規(guī)格 價格 是否有貨 數量
10 mM * 1 mL in Water ¥715
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1 mg ¥203
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5 mg ¥406
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10 mg ¥650
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50 mg ¥1989
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100 mg ¥3526
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Customer Review

Other Forms of Plerixafor octahydrochloride:

MCE 顧客使用本產品發(fā)表的 67 篇科研文獻

RT-PCR
WB
IF
Proliferation Assay
IHC

    Plerixafor octahydrochloride 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 octahydrochloride 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 octahydrochloride 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 octahydrochloride 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 octahydrochloride 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 octahydrochloride 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 octahydrochloride 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 octahydrochloride 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 octahydrochloride 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 octahydrochloride 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 octahydrochloride 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 octahydrochloride 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.

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    • 生物活性

    • 實驗參考方法

    • 純度 & 產品資料

    • 參考文獻

    生物活性

    Plerixafor octahydrochloride (AMD3100 octahydrochloride) is a selective CXCR4 antagonist with an IC50 of 44 nM.

    IC50 & Target[1][5]

    125I-CXCL12-CXCR4

    44 nM (IC50)

    125I-CXCL12-CXCR7

     

    HIV-1

    1-10 nM (EC50)

    HIV-2

    1-10 nM (EC50)

    細胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    CHO IC50
    0.26 μM
    Compound: 2, AMD3100
    Antagonist activity at human recombinant CXCR4 expressed in CHO cells assessed as inhibition of SDF1a-induced electrical impedance by dielectric spectroscopic analysis
    Antagonist activity at human recombinant CXCR4 expressed in CHO cells assessed as inhibition of SDF1a-induced electrical impedance by dielectric spectroscopic analysis
    [PMID: 22909088]
    CHO-K1 IC50
    > 100 μM
    Compound: 2, AMD3100
    Inhibition of human ERG expressed in CHOK1 cells after 5 mins by whole-cell patch clamp assay
    Inhibition of human ERG expressed in CHOK1 cells after 5 mins by whole-cell patch clamp assay
    [PMID: 22909088]
    MT4 EC50
    0.002 μM
    Compound: 2, AMD3100
    Antiviral activity against HIV1 infected in MT4 cells expressing CXCR4 assessed as inhibition of virus-induced cytopathic effect after 5 days
    Antiviral activity against HIV1 infected in MT4 cells expressing CXCR4 assessed as inhibition of virus-induced cytopathic effect after 5 days
    [PMID: 22909088]
    U-87MG ATCC IC50
    695 nM
    Compound: 1, AMD-3100
    Antagonist activity at human CXCR4 expressed in human U87 cells expressing CD4 assessed as inhibition of CXCL12-induced cAMP production pretreated for 15 mins before forskolin challenge by TR-FRET analysis
    Antagonist activity at human CXCR4 expressed in human U87 cells expressing CD4 assessed as inhibition of CXCL12-induced cAMP production pretreated for 15 mins before forskolin challenge by TR-FRET analysis
    [PMID: 21105715]
    體外研究
    (In Vitro)

    CXCR4 抑制劑 Plerixafor (AMD3100) 是一種有效的 CXCL12 介導趨化作用抑制劑 (IC50,5.7 nM),其效力略優(yōu)于其對 CXCR4 的親和力。用 CCX771 或 CXCL11 處理細胞對 CXCL12 介導的 MOLT-4 或 U937 TEM 沒有影響。相反,10 μM Plerixafor 可抑制兩種細胞系中 CXCL12 介導的 TEM[1]。與 CXCL12 刺激的細胞相比,Plerixafor (10 μM) 處理的細胞的細胞增殖有所減少,但未達到統(tǒng)計學意義[2]。

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

    體內研究
    (In Vivo)

    給 UUO 小鼠施用 Plerixafor (octahydrochloride) (2 mg/kg) 會加劇腎間質 T 細胞浸潤,導致促炎細胞因子 IL-6IFN-γ 的產生增加,抗炎細胞因子 IL-10 的表達減少[3]
    CXCR4 拮抗劑 Plerixafor (octahydrochloride) (AMD3100) 在 8 周時顯著降低血管周圍和間質纖維化[4]。LD50,小鼠,SC:16.3 mg/kg;LD50,大鼠,SC:>50 mg/kg;LD50,小鼠和大鼠,靜脈注射:5.2 mg/kg。

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

    Clinical Trial
    分子量

    794.47

    Formula

    C28H54N8.8HCl

    CAS 號
    性狀

    固體

    顏色

    White to yellow

    中文名稱

    鹽酸普樂沙福; 普樂沙福鹽酸鹽

    運輸條件

    Room temperature in continental US; may vary elsewhere.

    儲存方式

    4°C, sealed storage, away from moisture

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

    溶解性數據
    細胞實驗: 

    H2O 中的溶解度 : 100 mg/mL (125.87 mM; 超聲助溶)

    DMSO 中的溶解度 : < 1 mg/mL (insoluble or slightly soluble)

    配制儲備液
    濃度 溶劑體積 質量 1 mg 5 mg 10 mg
    1 mM 1.2587 mL 6.2935 mL 12.5870 mL
    5 mM 0.2517 mL 1.2587 mL 2.5174 mL
    查看完整儲備液配制表

    * 請根據產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復凍融造成的產品失效。
    儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲存時,請在6個月內使用,-20°C儲存時,請在1個月內使用。

    * 備注:如您選擇水作為儲備液,請稀釋至工作液后,再用 0.22 μm 的濾膜過濾除菌后使用。

    • 摩爾計算器

    • 稀釋計算器

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

    質量
    =
    濃度
    ×
    體積
    ×
    分子量 *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    濃度 (start)

    C1

    ×
    體積 (start)

    V1

    =
    濃度 (final)

    C2

    ×
    體積 (final)

    V2

    動物實驗:

    以下溶解方案,請直接配制工作液。建議現(xiàn)用現(xiàn)配,在短期內盡快用完。 以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比; 如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的方式助溶。

    • 方案 一

      請依序添加每種溶劑: PBS

      Solubility: 120 mg/mL (151.04 mM); 澄清溶液; 超聲助溶

    動物溶解方案計算器
    請輸入動物實驗的基本信息:

    給藥劑量

    mg/kg

    動物的平均體重

    g

    每只動物的給藥體積

    μL

    動物數量

    由于實驗過程有損耗,建議您多配一只動物的量
    計算結果
    工作液所需濃度 : mg/mL
    該產品水溶性佳,請具體參考實測 水 / PBS / Saline 中的溶解度數據。
    您所需的儲備液濃度超過該產品的實測溶解度,如有需要,請與 MCE 中國技術支持聯(lián)系。
    純度 & 產品資料
    參考文獻
    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, as described in the previous “Treatments” section. 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.

    參考文獻

    完整儲備液配制表

    * 請根據產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復凍融造成的產品失效。
    儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲存時,請在6個月內使用,-20°C儲存時,請在1個月內使用。

    可選溶劑 濃度 溶劑體積 質量 1 mg 5 mg 10 mg 25 mg
    H2O 1 mM 1.2587 mL 6.2935 mL 12.5870 mL 31.4675 mL
    5 mM 0.2517 mL 1.2587 mL 2.5174 mL 6.2935 mL
    10 mM 0.1259 mL 0.6294 mL 1.2587 mL 3.1468 mL
    15 mM 0.0839 mL 0.4196 mL 0.8391 mL 2.0978 mL
    20 mM 0.0629 mL 0.3147 mL 0.6294 mL 1.5734 mL
    25 mM 0.0503 mL 0.2517 mL 0.5035 mL 1.2587 mL
    30 mM 0.0420 mL 0.2098 mL 0.4196 mL 1.0489 mL
    40 mM 0.0315 mL 0.1573 mL 0.3147 mL 0.7867 mL
    50 mM 0.0252 mL 0.1259 mL 0.2517 mL 0.6294 mL
    60 mM 0.0210 mL 0.1049 mL 0.2098 mL 0.5245 mL
    80 mM 0.0157 mL 0.0787 mL 0.1573 mL 0.3933 mL
    100 mM 0.0126 mL 0.0629 mL 0.1259 mL 0.3147 mL

    * 備注:如您選擇水作為儲備液,請稀釋至工作液后,再用 0.22 μm 的濾膜過濾除菌后使用。

    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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    產品名稱:
    Plerixafor octahydrochloride
    目錄號:
    HY-50912
    需求量: