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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
CAS: 155148-31-5
产品质控
批次：
纯度：
99.77%
99.77
Plerixafor (AMD3100) 8HCl相关产品
| 相关靶点 | CXCR1 CXCR2 CXCR4 CXCR3 | 点击展开 |
|---|---|---|
| 相关产品 | SB225002 WZ811 Reparixin (Repertaxin) LIT-927 Navarixin (SCH-527123) UNBS5162 AMD3465 hexahydrobromide LY2510924 Danirixin (GSK1325756) MSX-122 AZD5069 SX-682 AMG 487 | 点击展开 |
| 相关化合物库 | FDA药物库 天然产物库 已知活性药物库-I GPCR小分子化合物库 | 点击展开 |
相关信号通路图
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(PMID) |
|---|---|---|---|---|---|
| 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 |
|
| 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] |
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|---|---|---|---|---|
| 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 |
|---|---|---|---|---|---|
| NCT05421416 | Not yet recruiting | Stem Cell Transplant Complications |
AHS Cancer Control Alberta |
April 1 2024 | Phase 2 |
| NCT05343572 | Recruiting | Asherman Syndrome|Atrophic Endometrium|Recurrent Implantation Failure |
Hugh Taylor|Yale University |
November 1 2023 | Early Phase 1 |
| 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 |
Ensoma|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 |
Water : 100 mg/mL (125.87 mM) 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 |
|
体内溶解配方 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
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
只
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，注：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：取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：取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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