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Plerixafor

Plerixafor

产品编号 T1776   CAS 110078-46-1
别名: 普乐沙福, JM3100, AMD 3100, AMD-3329

Plerixafor (AMD-3329) 是一种趋化因子受体拮抗剂,可阻断基质细胞衍生因子与细胞受体 CXCR4 的结合。它也是 CXCR7 的变构激动剂,是免疫刺激剂和造血干细胞动员剂,还抑制HIV-1和HIV-2的复制,EC50为 1-10 nM。

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Plerixafor Chemical Structure
Plerixafor, CAS 110078-46-1
规格 价格/CNY 货期 数量
1 mg ¥ 163 现货
5 mg ¥ 343 现货
10 mg ¥ 572 现货
25 mg ¥ 982 现货
50 mg ¥ 1,680 现货
100 mg ¥ 2,960 现货
200 mg ¥ 4,280 现货
500 mg ¥ 6,550 现货
其他形式的 Plerixafor:
产品目录号及名称: Plerixafor (T1776)
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纯度: 100%
纯度: 99.17%
纯度: 98%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Plerixafor (AMD-3329), a chemokine receptor antagonist, blocks the binding of stromal cell-derived factor (SDF-1alpha) to the cellular receptor CXCR4.
靶点活性 CXCR4:44 nM, CXCL12:5.7 nM
体外活性 Plerixafor inhibits CXCL12-mediated chemotaxis with a potency lightly better than its affinity for CXCR4. [1] Plerixafor also antagonizes SDF-1/CXCL12 ligand binding with an IC50 of 651 nM. Plerixafor inhibits SDF-1 mediated GTP-binding, SDF-1 mediated calcium flux and SDF-1 stimulated chemotaxis with IC50 of 27 nM, 572 nM and 51 nM, respectively. Plerixafor does not inhibit calcium flux against cells expressing CXCR3, CCR1, CCR2b, CCR4, CCR5 or CCR7 when stimulated with their cognate ligands, nor does Plerixafor inhibit receptor binding of LTB4. Plerixafor does not, on its own, induce a calcium flux in the CCRF–CEM cells, which express multiple GPCRs including CXCR4, CCR4 and CCR7. [2]
体内活性 A single topical application of Plerixafor promotes wound healing in diabetic mice by increasing cytokine production, mobilizing bone marrow EPCs, and enhancing the activity of fibroblasts and monocytes/macrophages, thereby increasing both angiogenesis and vasculogenesis. [3] Cohorts of mice are administered with PBS, IGF1, PDGF, SCF, or VEGF for five consecutive days and Plerixafor on the 5th day. The number and size of the colonies are highest in IGF1 plus Plerixafor injected mice compared to PDGF, SCF and VEGF treated groups, in combination with Plerixafor. [4]
激酶实验 In vitro biochemical assays against histone acetylases: GSK503 is profiled to assess inhibition against a panel of histone acetylases. GSK503 is dissolved in DMSO and tested in 10-dose IC50 mode with 3-fold serial dilution starting at 100 μM, with a final DMSO concentration of 2%. Anacardic Acid is used as positive control for CBP, GCN5, and pCAF and tested in 10-dose IC50 mode with 3-fold serial dilution starting at 100 μM. Curcumin is used as positive control for KAT5, MYST2/KAT7, MYST4/KAT6B, and p300, and tested in 10-dose IC50 mode with 3-fold serial dilution starting at 100 μM. Reactions are carried out at 3.08 μM Acetyl-CoA. For CBP, GCN5, MYST2/KAT7, pCAF, and p300, the substrate used is histone H3. For KAT5 and MYST4/KAT6B the substrates used are histone H2A and histone H4, respectively.
细胞实验 Plerixafor is dissolved in DMSO and then diluted with appropriate medium[2]. U87 mg 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].
别名 普乐沙福, JM3100, AMD 3100, AMD-3329
分子量 502.78
分子式 C28H54N8
CAS No. 110078-46-1

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

PBS: 1mg/mL (1.98 mM), sonification is recommended

Ethanol: 50 mg/mL, sonification is recommended.

DMSO: 2 mM, Sonification is recommeded

H2O: Insoluble

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
PBS / DMSO 1 mM 1.9889 mL 9.9447 mL 19.8894 mL 49.7235 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Zabel BA, et al. J Immunol. 2009, 183(5), 3204-3211. 2. Fricker SP, et al. Biochem Pharmacol. 2006, 72(5), 588-596. 3. Nishimura Y, et al. J Invest Dermatol. 2012, 132(3 Pt 1), 711-720. 4. Kumar S, et al. Bone. 2012, 50(4), 12012-12018. 5. Wei He, et al. Targeting CXC motif chemokine receptor 4 inhibits the proliferation, migration and angiogenesis of lung cancer cells. Oncol Lett. 2018 Sep;16(3):3976-3982. 6. Mercurio L, et al. Targeting CXCR4 by a selective peptide antagonist modulates tumor microenvironment and microglia reactivity in a human glioblastoma model. J Exp Clin Cancer Res. 2016 Mar 25;35:55. 7. Yang J, et al. Continuous AMD3100 Treatment Worsens Renal Fibrosis through Regulation of Bone Marrow Derived Pro-Angiogenic Cells Homing and T-Cell-Related Inflammation. PLoS One. 2016 Feb 22;11(2):e0149926. 8. He G, et al. SDF-1 in Mammary Fibroblasts of Bovine with Mastitis Induces EMT and Inflammatory Response of Epithelial Cells. Int J Biol Sci. 2017 May 5;13(5):604-614. 9. Dong L, Shen S, Chen W, et al. Discovery of Novel Inhibitors Targeting Human O-GlcNAcase: Docking-Based Virtual Screening, Biological Evaluation, Structural Modification, and Molecular Dynamics Simulation[J]. Journal of chemical information and modeling. 2019, 59(10): 4374-4382.

文献引用

1. Dong L, Shen S, Chen W, et al. Discovery of Novel Inhibitors Targeting Human O-GlcNAcase: Docking-Based Virtual Screening, Biological Evaluation, Structural Modification, and Molecular Dynamics Simulation. Journal of chemical information and modeling. 2019, 59(10): 4374-4382.
Aspirin L-Lysine hydrochloride NS2B-NS3pro-IN-1 NS2B-NS3pro-IN-2 ESI-09 A2ti-1 β-Herpesvirus protease-IN-1 Tubacin

相关化合物库

该产品包含在如下化合物库中:
抗癌药物库 抗癌活性化合物库 抗癌上市药物库 抗癌临床化合物库 药物功能重定位化合物库 抗病毒库 已知活性化合物库 GPCR靶点分子库 人代谢物化合物库 FDA上市及药典收录分子库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
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% Tween 80
% ddH2O
计算 重置

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Plerixafor 110078-46-1 Autophagy GPCR/G Protein Immunology/Inflammation Microbiology/Virology Proteases/Proteasome Virus Protease HIV Protease CXCR JM 3100 stream inhibit multiple Inhibitor SID-791 Human immunodeficiency virus cancer G-CSF 普乐沙福 human JM-3100 stem myeloma JM3100 SID 791 cells blood AMD 3100 CXC chemokine receptors lymphoma AMD3100 SID791 HIV ligand AMD 3329 AMD3329 AMD-3329 mobilizer peripheral AMD-3100 inhibitor

 

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