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Plerixafor (AMD3100) 8HCl

別名: JM 3100 8HCl,Plerixafor Octahydrochloride,AMD3100 octahydrochloride,SID791 octahydrochloride 中文名稱：普樂沙福八鹽酸鹽

Plerixafor (AMD3100, JM 3100,Plerixafor Octahydrochloride,AMD3100 octahydrochloride,SID791 octahydrochloride) 8HCl 是Plerixafor的鹽酸鹽，是CXCR4趨化因子受體拮抗劑，作用于CXCR4和CXCL12介導(dǎo)調(diào)節(jié)的趨化性，IC50分別為44 nM和5.7 nM。Plerixafor 可應(yīng)用為抗HIV的藥物。

Plerixafor (AMD3100) 8HCl Chemical Structure

Plerixafor (AMD3100) 8HCl Chemical Structure

CAS: 155148-31-5

規(guī)格 價格 庫存 購買數(shù)量
10mg 745.76 現(xiàn)貨
50mg 2193.41 現(xiàn)貨
1g 17772.3 現(xiàn)貨
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Plerixafor (AMD3100) 8HCl相關(guān)產(chǎn)品

相關(guān)信號通路圖

CXCR Signaling Pathways

CXCR信號通路圖

細胞實驗數(shù)據(jù)示例

細胞系 實驗類型 給藥濃度 孵育時間 活性描述 文獻信息
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
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生物活性

產(chǎn)品描述 Plerixafor (AMD3100, JM 3100,Plerixafor Octahydrochloride,AMD3100 octahydrochloride,SID791 octahydrochloride) 8HCl 是Plerixafor的鹽酸鹽，是CXCR4趨化因子受體拮抗劑，作用于CXCR4和CXCL12介導(dǎo)調(diào)節(jié)的趨化性，IC50分別為44 nM和5.7 nM。Plerixafor 可應(yīng)用為抗HIV的藥物。
靶點
CXCL12 [1]
(Cell-free assay)		 CXCR4 [1]
(Cell-free assay)
5.7 nM 44 nM
體外研究(In Vitro)
體外研究活性

Plerixafor 8HCl (AMD3100 8HCl)抑制CXCL12調(diào)節(jié)的趨化性，比作用于CXCR4親和力略高。[1] Plerixafor 8HCl (AMD3100 8HCl)也抑制SDF-1/CXCL12 配體結(jié)合，IC50為 651 nM。Plerixafor 8HCl (AMD3100 8HCl)抑制 SDF-1調(diào)節(jié)的GTP結(jié)合, SDF-1 調(diào)節(jié)的鈣流，和 SDF-1調(diào)節(jié)的趨化性，IC50分別為27 nM, 572 nM 和51 nM。Plerixafor作用于表達CXCR3, CCR1, CCR2b, CCR4, CCR5 或 CCR7的細胞，當被他們的同源配體刺激時，不抑制鈣流。Plerixafor 8HCl (AMD3100 8HCl)也不抑制 LTB4的受體結(jié)合。Plerixafor 8HCl (AMD3100 8HCl)作用于表達多種GPCRs，包括CXCR4,CCR4 和 CCR7的CCRF-CEM細胞，不會有的鈣流。[2]
實驗圖片 檢測方法 檢測指標 實驗圖片 PMID
Immunofluorescence CXCR4 β-arrestin2 28521261
體內(nèi)研究(In Vivo)
體內(nèi)研究活性

Plerixafor單獨局部處理，通過提高細胞因子產(chǎn)量，調(diào)動骨髓EPCs, 和增強成纖維細胞和單核細胞/巨噬細胞的活性,因此提高血管生成，而促進糖尿病小鼠傷口愈合。[3]
動物實驗 Animal Models 12周大的節(jié)段性骨缺損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 --

化學(xué)信息&溶解度

分子量 794.47 分子式

C28H54N8.8HCl
CAS號 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
儲存條件(自收到貨起)

體外溶解度
批次：

Water : 100 mg/mL (125.87 mM)

DMSO : Insoluble ( ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Ethanol : Insoluble

摩爾濃度計算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑

 動物體內(nèi)配方計算器

實驗計算

摩爾濃度計算器

質(zhì)量 濃度 體積 分子量

動物體內(nèi)配方計算器（澄清溶液）

第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）

mg/kg g μL 只

第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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