Plerixafor (AMD3100) 8HCl

别名: JM 3100 8HCl,Plerixafor Octahydrochloride,AMD3100 octahydrochloride,SID791 octahydrochloride 中文名称:普乐沙福八盐酸盐

Plerixafor (AMD3100, JM 3100,Plerixafor Octahydrochloride,AMD3100 octahydrochloride,SID791 octahydrochloride) 8HCl 是Plerixafor的盐酸盐,是CXCR4趋化因子受体拮抗剂,作用于CXCR4和CXCL12介导调节的趋化性,IC50分别为44 nM和5.7 nM。Plerixafor 可应用为抗HIV的药物。

Plerixafor (AMD3100) 8HCl Chemical Structure

Plerixafor (AMD3100) 8HCl Chemical Structure

CAS: 155148-31-5

规格 价格 库存 购买数量
10mg RMB 745.76 现货
50mg RMB 2193.41 现货
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客户使用Selleck的Plerixafor (AMD3100) 8HCl发表文献44

产品质控

批次: 纯度: 99.77%
99.18

Plerixafor (AMD3100) 8HCl相关产品

相关信号通路图

CXCR抑制剂选择性比较

细胞实验数据示例

细胞系 实验类型 给药浓度 孵育时间 活性描述 文献信息
human MT2 cells Function assay 1 ug/mL 4 days Antiviral activity against HIV1 3B infected in human MT2 cells assessed as inhibition of viral p24 antigen production at 1 ug/mL after 4 days by ELISA 21168336
human MOLT4 cells Function assay 1000 nM Inhibition of Mab 12G5 binding to CXCR4 expressed in human MOLT4 cells at 1000 nM by FACS analysis 19451305
human U87 cells Function assay 1000 nM Antagonist activity at CXCR4 in human U87 cells assessed as inhibition of SDF1-induced modulation of cAMP production at 1000 nM by TR-FRET assay 17958344
human MT4 cells Function assay 4 days Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus replication after 4 days by MTT assay, EC50=4 nM 20043638
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
U87 Function assay 15 mins 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, IC50=0.695μM 21105715
MT4 Antiviral assay 5 days Antiviral activity against HIV1 infected in MT4 cells expressing CXCR4 assessed as inhibition of virus-induced cytopathic effect after 5 days, EC50=0.002μM 22909088
CD44null Function assay 7 days Effect on human GBM2 cell differentiation assessed as increase in CD44null cells after 7 days by flow cytometric analysis 22909088
CD44null Function assay 7 days Effect on human GBM1 cell differentiation assessed as increase in CD44null cells after 7 days by flow cytometric analysis 22909088
CEM-SS cells Function assay Effective concentration of compound against HIV-1 LAI strain in CEM-SS cells, EC50=127 nM 14698189
rat IR983F cells Function assay Displacement of [125I]CXCL12 from CXCR4 in rat IR983F cells, IC50=108 nM 19053768
MT-4 cells Function assay Effective concentration of compound against HIV-1 IIIB strain in MT-4 cells, EC50=65 nM 14698189
human Jurkat cells Function assay Antagonist activity at CXCR4 in human Jurkat cells assessed as inhibition of SDF1-induced cell migration, IC50=27.4 nM 19188071
PBMC cells Function assay Effective concentration of compound against HIV-1 89.6 strain in PBMC cells, EC50=3.8 nM 14698189
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
CHOK1 cells Function assay Displacement of [125I]SDF1alpha from CXCR4 expressed in CHOK1 cells, IC50=0.81 nM 17715128
human HL60 cells Function assay Displacement of [125I]SDF1alpha from CXCR4 in human HL60 cells, IC50=15.2 μM 19188071
MT4 Antiviral assay Antiviral activity against HIV1 3B assessed as reduction in cytopathic effect in MT4 cells, EC50=0.011μM 17034122
MT4 Antiviral assay Antiviral activity against X4-tropic HIV1 NL4.3 infected in human MT4 cells assessed as protection from virus-induced cytopathogenicity, EC50=0.062μM 22579418
CHO Function assay Binding affinity to human recombinant CXCR4 expressed in CHO cells, Kb=0.077μM 22909088
CHO Function assay Antagonist activity at human recombinant CXCR4 expressed in CHO cells assessed as inhibition of SDF1a-induced electrical impedance by dielectric spectroscopic analysis, IC50=0.26μM 22909088
点击查看更多细胞系数据

生物活性

产品描述 Plerixafor (AMD3100, JM 3100,Plerixafor Octahydrochloride,AMD3100 octahydrochloride,SID791 octahydrochloride) 8HCl 是Plerixafor的盐酸盐,是CXCR4趋化因子受体拮抗剂,作用于CXCR4和CXCL12介导调节的趋化性,IC50分别为44 nM和5.7 nM。Plerixafor 可应用为抗HIV的药物。
靶点
CXCL12 [1]
(Cell-free assay)
CXCR4 [1]
(Cell-free assay)
5.7 nM 44 nM
体外研究(In Vitro)
体外研究活性

Plerixafor 8HCl (AMD3100 8HCl)抑制CXCL12调节的趋化性,比作用于CXCR4亲和力略高。[1] Plerixafor 8HCl (AMD3100 8HCl)也抑制SDF-1/CXCL12 配体结合,IC50为 651 nM。Plerixafor 8HCl (AMD3100 8HCl)抑制 SDF-1调节的GTP结合, SDF-1 调节的钙流,和 SDF-1调节的趋化性,IC50分别为27 nM, 572 nM 和51 nM。Plerixafor作用于表达CXCR3, CCR1, CCR2b, CCR4, CCR5 或 CCR7的细胞,当被他们的同源配体刺激时,不抑制钙流。Plerixafor 8HCl (AMD3100 8HCl)也不抑制 LTB4的受体结合。Plerixafor 8HCl (AMD3100 8HCl)作用于表达多种GPCRs,包括CXCR4,CCR4 和 CCR7的CCRF-CEM细胞,不会有的钙流。[2]

实验图片 检测方法 检测指标 实验图片 PMID
Immunofluorescence CXCR4 β-arrestin2 28521261
体内研究(In Vivo)
体内研究活性

Plerixafor单独局部处理,通过提高细胞因子产量,调动骨髓EPCs, 和增强成纤维细胞和单核细胞/巨噬细胞的活性,因此提高血管生成,而促进糖尿病小鼠伤口愈合。[3]

动物实验 Animal Models 12周大的节段性骨缺损C57BL/6 小鼠
Dosages 5 mg/kg
Administration 腹腔注射
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05343572 Recruiting
Asherman Syndrome|Atrophic Endometrium|Recurrent Implantation Failure
Hugh Taylor|Yale University
November 1 2023 Early Phase 1
NCT05421416 Not yet recruiting
Stem Cell Transplant Complications
AHS Cancer Control Alberta
November 1 2023 Phase 2
NCT05844527 Recruiting
Wound of Skin|Abdominal Wound
MedRegen LLC
November 20 2023 Phase 2
NCT05411575 Withdrawn
COVID-19 Acute Respiratory Distress Syndrome|COVID-19
4Living Biotech|4P-Pharma
July 19 2022 Phase 2
NCT05445128 Terminated
Sickle Cell Disease
Magenta Therapeutics Inc.|bluebird bio
June 24 2022 Phase 2
NCT05835726 Recruiting
Multiple Myeloma|Daratumumab|Autologous Stem Cell Transplantation|Leukapheresis
Fondazione Policlinico Universitario Agostino Gemelli IRCCS
January 1 2022 --

化学信息&溶解度

分子量 794.47 分子式

C28H54N8.8HCl

CAS号 155148-31-5 SDF Download Plerixafor (AMD3100) 8HCl SDF
Smiles C1CNCCNCCCN(CCNC1)CC2=CC=C(C=C2)CN3CCCNCCNCCCNCC3.Cl.Cl.Cl.Cl.Cl.Cl.Cl.Cl
储存条件(自收到货起)

体外溶解度
批次:

Water : 100 mg/mL

DMSO : Insoluble ( DMSO吸湿会降低化合物溶解度,请使用新开封DMSO)

Ethanol : Insoluble

摩尔浓度计算器

体内溶解度
批次:

现配现用,请按从左到右的顺序依次添加,澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量 浓度 体积 分子量

动物体内配方计算器(澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)

mg/kg g μL

第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)

% DMSO % % Tween 80 % ddH2O
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

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