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普乐沙福 /Plerixafor {[allProObj[0].p_purity_real_show]}

货号:A195007 同义名: AMD 3100;JM3100

Plerixafor is a chemokine receptor antagonist for CXCR4 and CXCL12-mediated chemotaxis with IC50 of 44 nM and 5.7 nM, respectively.

Plerixafor 化学结构 CAS号:110078-46-1
Plerixafor 化学结构
CAS号:110078-46-1
Plerixafor 3D分子结构
CAS号:110078-46-1
Plerixafor 化学结构 CAS号:110078-46-1
Plerixafor 3D分子结构 CAS号:110078-46-1
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Plerixafor 纯度/质量文件 产品仅供科研

货号:A195007 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 CXCR1 CXCR2 CXCR4 其他靶点 纯度
Reparixin 99%+
SB225002 +++

CXCR2, IC50: 22 nM

99%+
Plerixafor ++

CXCR4, IC50: 44 nM

99%
AMD 3465 6HBr 98%
WZ811 ++++

CXCR4, EC50: 0.3 nM

98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Plerixafor 生物活性

靶点
  • CXCR4

    CXCR4, IC50:44 nM

描述 Through binding with CC- and CXC-chemokines, CCR and CXCR, the subsets of the chemokine receptor family can trigger an intracellular signal transduction cascade, thus mediating the recruitment of immune cells to the in£ammation or infection sites and implicated in several immuno-related disease states, organogenesis, angiogenesis and tumor growth and metastasis. AMD3100 is a selective antagonist of CXCR4 with IC50 values ranging in 0.01-0.13μg/ml for antagonizing SDF-1, but not itself, activated calcium flux in different cells tested, including CXCR4-transfected U87 and CD4 cells, freshly isolated PBMCs, SupT1, THP-1, HSB-2, Molt-4 and L1210 cells. The inhibitory effect of AMD3100 against the induced endocytosis of CXCR4 is selectively SDF-1-dependent but not phorbol ester. Pre-incubated with AMD3100 at concentration of 0.04, 0.2, 1, 5 and 25μg/ml could dose-dependently inhibit the SDF-1-induced (200 ng/ml) chemotaxis of human PBMCs[1]. In vivo study showed that intraperitoneal injection with 5mg/kg AMD3100 can alter the potential of mesenchymal stem cells mobilization induced by different growth factors, including IGF-1, SCF, PDGF and VEGF, in mice, which may be mediated through Akt/PI3K, MEK1/2-Erk1/2 and smad2/3 as key signaling pathways[2].
作用机制 Not found

Plerixafor 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
CEM-SS cells Function assay Effective concentration of compound against HIV-1 LAI strain in CEM-SS cells, EC50=127 nM 14698189
CHOK1 cells Function assay Displacement of [125I]SDF1alpha from CXCR4 expressed in CHOK1 cells, IC50=0.81 nM 17715128
GHOST CXCR4 cell line Function assay Inhibitory concentration of compound against HIV-1 LAI strain in GHOST CXCR4 cell line, IC50=0.95 nM 14698189
HEK293 cells Function assay 2 days Antiviral activity against T20-resistant HIV1 NL4-3 infected in HEK293 cells assessed as inhibition of viral replication after 2 days, IC50=2.3 nM 19451305

Plerixafor 动物研究

Dose Mice[3]: 0.625 mg/kg - 10 mg/kg (s.c.) Rat[3]: 25 mg/kg (s.c.), 2 mg/kg (i.v.)
Administration s.c., i.v.
Pharmacokinetics
Animal Rats[3]
Dose 1 mg/kg
Administration s.c.
T1/2 0.1 h (absorption)
Tmax 0.5 h
AUC0-7 5410 pmol·h/ml
Cmax 3082 pmol/ml
t1/2λ1 0.9 h
AUC 5444 pmol·h/ml

Plerixafor 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01164475 - Completed - -
NCT01711073 End Stage Liver DIsease Phase 1 Unknown September 2013 United States, New Jersey ... 展开 >> University of Medicine and Dentistry of New Jersey Recruiting Newark, New Jersey, United States, 07101 Contact: Baburao Koneru, MD       koneruba@umdnj.edu 收起 <<
NCT01123499 - Recruiting - United States, Maryland ... 展开 >> National Institutes of Health Clinical Center, 9000 Rockville Pike Recruiting Bethesda, Maryland, United States, 20892 Contact: Sandra Maxwell, B.S.N.    301-402-1773    maxwells@niaid.nih.gov 收起 <<

Plerixafor 参考文献

[1]Plerixafor

Plerixafor 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.99mL

0.40mL

0.20mL

9.94mL

1.99mL

0.99mL

19.89mL

3.98mL

1.99mL

Plerixafor 技术信息

CAS号110078-46-1
分子式C28H54N8
分子量 502.78
别名 AMD 3100;JM3100;JKL 169;Mozobil;SDZ SID 791;SID791
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,2-8°C

溶解度

DMSO: 1.5 mg/mL(2.98 mM),配合低频超声,水浴加热至45℃,并调节pH至5,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

无水乙醇: 45 mg/mL(89.5 mM),配合低频超声助溶,注意:无水乙醇开封后,易挥发,也会吸收空气中的水分,导致溶解能力下降,请避免使用开封较久的乙醇

动物实验配方

PO 0.5% CMC-Na 30 mg/mL suspension

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