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  4. AMD 3465 hexahydrobromide

AMD 3465 hexahydrobromide  (Synonyms: GENZ-644494 hexahydrobromide)

目录号: HY-15971 纯度: ≥98.0%
COA 产品使用指南

摩尔计算器

AMD 3465 hexahydrobromide (GENZ-644494 hexahydrobromide) 是一种有效的 CXCR4 拮抗剂，在 SupT1 细胞中，能够抑制 12G5 mAb，CXCL12AF647 与 CXCR4 的结合，IC50 值分别为 0.75 nM 和 18 nM；AMD 3465 同时可有效抑制 X4 HIV 的复制 (IC50，1-10 nM)，但对 R5 HIV 病毒无作用。

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AMD 3465 hexahydrobromide Chemical Structure

AMD 3465 hexahydrobromide Chemical Structure

CAS No. : 185991-07-5

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规格 价格 是否有货 数量
Free Sample (0.1 - 0.2 mg)   Apply now  
10 mM * 1 mL in DMSO ￥790
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5 mg ￥550
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10 mg ￥800
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50 mg ￥2600
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100 mg ￥4800
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500 mg   询价  

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Customer Review

Other Forms of AMD 3465 hexahydrobromide:

AMD 3465 hexahydrobromide 相关抗体

Top Publications Citing Use of Products

    AMD 3465 hexahydrobromide purchased from MCE. Usage Cited in: Biomed Pharmacother. 2021 Mar 24;138:111476.  [Abstract]

    The results of western blotting showed that high glucose inhibited the activation of the cell cycle pathway, the expression level of CDK4, CDK6, Nusap1, and Cyclin D1 are reduced. However, under the action of AMD3465 (10 μM), the expression level of proteins is significantly higher than that of the HG group.

    查看 CXCR 亚型特异性产品:

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    CXCR CXCR1 CXCR2 CXCR3 CXCR4 CXCR7 CXCR6

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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

    AMD 3465 hexahydrobromide (GENZ-644494 hexahydrobromide) is a potent antagonist of CXCR4, inhibits binding of 12G5 mAb and CXCL12AF647 to CXCR4, with IC50s of 0.75 nM and 18 nM in SupT1 cells; AMD 3465 also potently inhibits the replication of X4 HIV strains (IC50: 1-10 nM), but has no effect on CCR5-using (R5) viruses.

    IC50 & Target[1]

    12G5 mAb-CXCR4

    0.75 nM (IC50, in SupT1 cells)

    CXCL12AF647-CXCR4

    18 nM (IC50, in SupT1 cells)

    X4 HIV-1 (NL4.3)

    6.1 nM (IC50, in MT-4 cells)

    X4 HIV-1 (RF)

    7.4 nM (IC50, in MT-4 cells)

    X4 HIV-1 (HE)

    9.8 nM (IC50, in MT-4 cells)

    X4 HIV-1 (IIIB)

    12.3 nM (IC50, in MT-4 cells)

    X4 HIV-1 (NL4.3AMD3100)

    2822 nM (IC50, in MT-4 cells)

    HIV-2 (ROD)

    12.3 nM (IC50, in MT-4 cells)

    HIV-2 (EHO)

    12.3 nM (IC50, in MT-4 cells)

    体外研究
    (In Vitro)

    AMD 3465 hexahydrobromide is a potent antagonist of CXCR4, inhibits binding of 12G5 mAb and CXCL12AF647 to CXCR4, with IC50s of 0.75 nM and 18 nM in SupT1 cells. AMD 3465 (50 nM) totally blocks CXCL12-induced calcium mobilization, with an IC50 of 17 nM, but shows no effect on the intracellular calcium fluxes elicited by the CCR5 ligands RANTES, LD78β and MIP-1β in U87.CD4.CCR5 cells. AMD 3465 also potently inhibits the replication of X4 HIV strains (IC50: 1-10 nM), but has no effect on CCR5-using (R5) viruses. AMD3465 is cytotoxic to the X4 HIV-1 strains IIIB, NL4.3, RF and HE with an IC50 ranging from 6 to 12 nM. The IC50 for suppression of the HIV-2 strains ROD and EHO is 12.3 nM[1]. AMD 3465 inhibits CXCL-12-induced growth in U87 and Daoy cells. AMD 3465 treatment stimulates the phosphorylation of Erk1/2 in U87 and Daoy cells[2].

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

    AMD 3465 hexahydrobromide 相关抗体:
    体内研究
    (In Vivo)

    AMD 3465 (2.5 mg/kg/d, s.c. for 5 weeks) significantly blocks the growth of U87 GBM and Daoy xenografts[2].

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

    896.07

    Formula

    C24H44Br6N6
    CAS 号
    性状

    固体

    颜色

    Light yellow to yellow

    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： 

    DMSO 中的溶解度 : 50 mg/mL (55.80 mM; 超声助溶; 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 : ≥ 38 mg/mL (42.41 mM)

    * "≥" means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 1.1160 mL 5.5799 mL 11.1598 mL
    5 mM 0.2232 mL 1.1160 mL 2.2320 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: ≥ 2.5 mg/mL (2.79 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 25.0 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% Corn Oil

      Solubility: ≥ 2.5 mg/mL (2.79 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。

      以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

    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: 100 mg/mL (111.60 mM); 澄清溶液; 超声助溶

    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
    计算结果
    工作液所需浓度 : mg/mL
    该产品水溶性佳，请具体参考实测 水 / PBS / Saline 中的溶解度数据。
    您所需的储备液浓度超过该产品的实测溶解度，如有需要，请与 MCE 中国技术支持联系。
    纯度 & 产品资料

    纯度: ≥98.0%

    COA (289 KB) HNMR (206 KB)

    产品使用指南 (1538 KB)
    参考文献
    Cell Assay
    [2]

    Following serum starvation for 24 h, astrocytes, granule cells, U87 cells, and Daoy cells are treated with 1 μg/mL CXCL12, 2.5 ng/mL AMD 3465, 200 μM rolipram, or 10 μM forskolin. Daoy and U87 cell growth in culture is measured by trypan blue exclusion after 24 and 48 h of treatment, respectively[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [2]

    Mice[2]
    Mice are imaged at least twice after implantation of cells to identify those with equivalent tumor growth rates. Two weeks after tumor cell implantation, cohorts of mice with approximately equivalent tumor bioluminescence are divided into equal control and treatment groups. Animals in AMD 3465 experiments receive s.c. osmotic pumps loaded with 10 mg/mL AMD 3465 in sterile PBS or PBS alone. The infusion rate is 0.25 μL/h (50 μg/d). For the experiments with rolipram or caffeine, mice in the treatment groups receive oral administration of rolipram (5 μg/g/d) or caffeine (100 μg/g/d). The concentration of drug in the water is determined from daily measurements of water consumption by each animal over the course of 7 days. Concentrations are adjusted based on water consumption to provide the prescribed dose[2].

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

    AMD 3465 hexahydrobromide 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
    H2O / DMSO 1 mM 1.1160 mL 5.5799 mL 11.1598 mL 27.8996 mL
    5 mM 0.2232 mL 1.1160 mL 2.2320 mL 5.5799 mL
    10 mM 0.1116 mL 0.5580 mL 1.1160 mL 2.7900 mL
    15 mM 0.0744 mL 0.3720 mL 0.7440 mL 1.8600 mL
    20 mM 0.0558 mL 0.2790 mL 0.5580 mL 1.3950 mL
    25 mM 0.0446 mL 0.2232 mL 0.4464 mL 1.1160 mL
    30 mM 0.0372 mL 0.1860 mL 0.3720 mL 0.9300 mL
    40 mM 0.0279 mL 0.1395 mL 0.2790 mL 0.6975 mL
    DMSO 50 mM 0.0223 mL 0.1116 mL 0.2232 mL 0.5580 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
    • 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.

    Keywords:

    AMD 3465 hexahydrobromide185991-07-5GENZ-644494 hexahydrobromideCXCRHIVCXC chemokine receptorsC-X-C motif chemokine receptorsHuman immunodeficiency virusInhibitorinhibitorinhibit

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