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Plerixafor (AMD3100)

別名: JM 3100, SID791 中文名稱：普樂沙福

Plerixafor (AMD3100, JM 3100, SID791)是一種趨化因子受體拮抗劑，作用于CXCR4和CXCL12介導(dǎo)的趨化性，無細(xì)胞試驗(yàn)中IC50分別為44 nM和5.7 nM。Plerixafor 可抑制human immunodeficiency virus (HIV)復(fù)制。

Plerixafor (AMD3100) Chemical Structure

Plerixafor (AMD3100) Chemical Structure

CAS: 110078-46-1

規(guī)格 價格 庫存 購買數(shù)量
5mg 814.08 現(xiàn)貨
10mg 1215.55 現(xiàn)貨
50mg 3866.09 現(xiàn)貨
1g 24488.1 現(xiàn)貨
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Plerixafor (AMD3100)相關(guān)產(chǎn)品

相關(guān)信號通路圖

CXCR Signaling Pathways

CXCR信號通路圖

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系 實(shí)驗(yàn)類型 給藥濃度 孵育時間 活性描述 文獻(xiàn)信息
MT2 Antiviral 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
TZM-bl Antiviral assay 100 uM 24 hrs Antiviral activity against HIV NL-Lai infected in human TZM-bl cells assessed as inhibition of viral infection at 100 uM treated before viral infection measured after 24 hrs by luciferase assay 21783371
MDA-MB-231 Function assay 100 nM 24 hrs Antagonist activity at CXCR4-mediated chemotaxis in human MDA-MB-231 cells assessed as inhibition of CXCL12-induced cell invasion at 100 nM after 24 hrs by crystal violet staining-based microscopic matrigel assay 29494843
CXCR4+ Function assay 6 mg/kg 2 hrs Induction hematopoietic stem cell mobilization in C57BL/6 mouse assessed as increase in CXCR4+ cells in blood at 6 mg/kg, sc measured after 2 hrs by APC-conjugated anti-CXCR4-staining based flow cytometry relative to vehicle control 29314840
U87 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
MOLT4 Function assay 1000 nM Inhibition of Mab 12G5 binding to CXCR4 expressed in human MOLT4 cells at 1000 nM by FACS analysis 19451305
Jurkat Function assay 0.01 to 100 uM Inhibition of CXCR4 in human Jurkat cells assessed as reduction in HIV-Nef-M1-induced mitochondrial membrane depolarization at 0.01 to 100 uM by JC1 dye based fluorescence depolarization assay 26191361
HEK293 Antiviral 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 = 0.0023 μM. 19451305
MT4 Antiviral assay 5 days Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay, EC50 = 0.002 μM. 26974376
MT4 Antiviral assay 5 days Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay, EC50 = 0.002 μM. 26974376
MT4 Antiviral 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 = 0.004 μM. 20043638
HEK293 Antiviral assay 2 days Antiviral activity against HIV1 NL4-3 infected in HEK293 cells assessed as inhibition of viral replication after 2 days, IC50 = 0.0046 μM. 19451305
HEK293 Antiviral assay 2 days Antiviral activity against multidrug resistant HIV1 HXB2 infected in HEK293 cells assessed as inhibition of viral replication after 2 days, IC50 = 0.0053 μM. 19451305
CEM-CCRF Function assay 30 mins Inhibition of PE-conjugated-12G5 anti-CXCR4 antibody binding to CXCR4 in human CEM-CCRF cells preincubated for 30 mins followed by antibody addition by FACS Canto II cytofluorometric analysis, IC50 = 0.006 μM. 27571038
HEK293 Antiviral assay 2 days Antiviral activity against HIV1 HXB2 infected in HEK293 cells assessed as inhibition of viral replication after 2 days, IC50 = 0.0062 μM. 19451305
HEK293 Antiviral assay 2 days Antiviral activity against NNRTI-resistant HIV1 HXB2 infected in HEK293 cells assessed as inhibition of viral replication after 2 days, IC50 = 0.007 μM. 19451305
HEK293 Antiviral assay 2 days Antiviral activity against NRTI-resistant HIV1 HXB2 infected in HEK293 cells assessed as inhibition of viral replication after 2 days, IC50 = 0.009 μM. 19451305
HEK293 Antiviral assay 2 days Antiviral activity against PI-resistant HIV1 HXB2 infected in HEK293 cells assessed as inhibition of viral replication after 2 days, IC50 = 0.0092 μM. 19451305
MT4 Antiviral assay 5 days Antiviral activity against T-cell line-tropic HIV1 NL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 5 days by MTT assay in presence of 5 uM of chloroquine, EC50 = 0.025 μM. 26094944
MT4 Antiviral assay 5 days Antiviral activity against T-cell line-tropic HIV1 NL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 5 days by MTT assay, EC50 = 0.032 μM. 26094944
MT4 Antiviral assay 5 days Antiviral activity against T-cell line-tropic HIV1 NL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 5 days by MTT assay in presence of 2.5 uM of chloroquine, EC50 = 0.039 μM. 26094944
HPBALL Function assay 3 hrs Displacement of 12G5-CXCL12 from CXCR4 in human HPBALL cells after 3 hrs by FACS analysis, IC50 = 0.29 μM. 29494843
MDA-MB-231 Function assay 10 mins Displacement of biotinylated TN14003 from CXCR4 CXCL12 binding domain in human MDA-MB-231 cells preincubated for 10 mins followed by biotinylated TN14003 addition measured after 30 mins using streptavidin-conjugated rhodamine by fluorescence microscopic a, EC = 1 μM. 27179215
MDA-MB-231 Function assay 10 mins Inhibition of biotinylated TN14003 binding to CXCR4 in human MDA-MB-231 cells preincubated for 10 mins followed by TN14003 addition measured after 30 mins by rhodamine dye-based microscopic analysis, EC = 1 μM. 29529500
MDA-MB-231 Function assay 10 mins Displacement of biotinylated-TN14003 from CXCR4 in human MDA-MB-231 cells assessed as reduction in fluorescence preincubated for 10 mins followed by biotinylated-TN14003 addition measured after 30 mins by streptavidin-rhodamine staining based microscopic , EC = 1 μM. 27914361
MDA-MB-231 Function assay 10 mins Inhibition of biotinylated TN14003 binding to CXCR4 in human MDA-MB-231 cells assessed as reduction in fluorescence preincubated for 10 mins followed by biotinylated-TN14003 addition measured after 30 mins by streptavidin-rhodamine staining based immunofl, EC = 1 μM. 28521261
CCRF-CEM Function assay 30 mins Inhibition of anti-CXCR4 PE antibody clone 12G5 binding to CXCR4 in human CCRF-CEM cells preincubated for 30 mins followed by anti-CXCR4 PE antibody clone 12G5 addition measured after 30 mins by flow cytometric method, IC50 = 6.2 μM. 29125295
TZM-bl Antiviral assay 1 hr Antiviral activity against HIV1 HXB2 pseudovirus infected in human TZM-bl cells assessed as inhibition of viral entry treated 1 hr post infection measured after 48 hrs by luciferase reporter gene assay 28266845
U87.CD4 Antiviral assay Antiviral activity against HIV1 clinical isolate 10 infected in U87.CD4 cells expressing human CXCR4 H281A mutant, IC50 = 0.0024 μM. 17599916
U87.CD4 Antiviral assay Antiviral activity against HIV1 NDK infected in U87.CD4 cells expressing human CXCR4 H281A mutant, IC50 = 0.0019 μM. 17599916
U87.CD4 Antiviral assay Antiviral activity against HIV1 NL43 infected in U87.CD4 cells expressing human CXCR4 H281A mutant, IC50 = 0.0019 μM. 17599916
CHOK1 Function assay Displacement of [125I]SDF1alpha from CXCR4 expressed in CHOK1 cells, IC50 = 0.00081 μM. 17715128
CHOK1 Function assay Displacement of [125I]MCP1 from CCR2/CXCR4 expressed in CHOK1 cells, IC50 = 0.00009 μM. 17715128
CHOK1 Function assay Displacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cells, IC50 = 0.00004 μM. 17715128
U87.CD4 Antiviral assay Antiviral activity against HIV1 clinical isolate 10 infected in U87.CD4 cells expressing human wild type CXCR4, IC50 = 0.003 μM. 17599916
PBMC Function assay Effective concentration of compound against HIV-1 89.6 strain in PBMC cells, EC50 = 0.0038 μM. 14698189
MT-4 Function assay Effective concentration against HIV-1(IIIB) replication in MT-4 cells, EC50 = 0.0042 μM. 8568797
MT-4 Function assay Effective concentration against HIV-2(ROD) replication in MT-4 cells, EC50 = 0.0059 μM. 8568797
U87.CD4 Antiviral assay Antiviral activity against HIV1 NDK infected in U87.CD4 cells expressing human wild type CXCR4, IC50 = 0.0076 μM. 17599916
MT-4 Antiviral assay Antiviral activity against HIV 1 RIN HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay after 40 passages selected in presence of compound, EC50 = 0.008 μM. 18378713
MT-4 Antiviral assay Antiviral activity against HIV 1 RIN HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay after 60 passages selected in presence of compound, EC50 = 0.008 μM. 18378713
MT-4 Antiviral assay Antiviral activity against HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay after 20 passages selected in presence of compound, EC50 = 0.008 μM. 18378713
U87.CD4 Antiviral assay Antiviral activity against HIV1 NL43 infected in U87.CD4 cells expressing human wild type CXCR4, IC50 = 0.014 μM. 17599916
MT-4 Antiviral assay Antiviral activity against HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay, EC50 = 0.014 μM. 18378713
U87.CD4 Antiviral assay Antiviral activity against HIV1 NDK infected in U87.CD4 cells expressing human CXCR4 D171N mutant, IC50 = 0.017 μM. 17599916
CD4+ T Function assay Antagonist activity at CXCR4 in human CD4+ T cells assessed as inhibition of CXCL12-mediated cytosolic calcium level preincubated with compounds followed by CXCL12 stimulation by calcium 4 dye-based FLIPR assay, IC50 = 0.018 μM. 29494843
U87.CD4 Antiviral assay Antiviral activity against HIV1 clinical isolate 10 infected in U87.CD4 cells expressing human CXCR4 D171N mutant, IC50 = 0.019 μM. 17599916
Jurkat Function assay Antagonist activity at CXCR4 in human Jurkat cells assessed as inhibition of SDF1-induced cell migration, IC50 = 0.0274 μM. 19188071
MT-4 Antiviral assay Antiviral activity against HIV 1 3B harboring integrase L34M mutant infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay selected after 40 passages in presence of compound, EC50 = 0.028 μM. 18378713
MT-4 Antiviral assay Antiviral activity against HIV 1 3B infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay, EC50 = 0.034 μM. 18378713
U87.CD4 Antiviral assay Antiviral activity against HIV1 NL43 infected in U87.CD4 cells expressing human CXCR4 D171N mutant, IC50 = 0.046 μM. 17599916
MT-4 Antiviral assay Antiviral activity against HIV 1 3B harboring integrase E92Q S230N double mutant infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay selected after 20 passages in presence of compound, EC50 = 0.049 μM. 18378713
MT-4 Antiviral assay Antiviral activity against HIV 1 3B harboring integrase E92Q, S230N and L34M triple mutant infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay selected after 60 passages in presence of compound, EC50 = 0.056 μM. 18378713
MT-4 Function assay Effective concentration of compound against HIV-1 IIIB strain in MT-4 cells, EC50 = 0.065 μM. 14698189
HEK293 Function assay Inhibition of Mab 12G5 binding to CXCR4 H281A mutant expressed in HEK293 cells, IC50 = 0.0727 μM. 19451305
IR983F Function assay Displacement of [125I]CXCL12 from CXCR4 in rat IR983F cells, IC50 = 0.108 μM. 19053768
CEM-SS Function assay Effective concentration of compound against HIV-1 LAI strain in CEM-SS cells, EC50 = 0.127 μM. 14698189
COS7 Function assay Antagonist activity at human CXCR4 V196A mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover, Ki = 0.14 μM. 17599916
HEK293 Function assay Inhibition of Mab 12G5 binding to CXCR4 D181A mutant expressed in HEK293 cells, IC50 = 0.1437 μM. 19451305
COS7 Function assay Displacement of [125I]12G5 antibody from transmembrane domain 7 of human CXCR4 H281A mutant expressed in COS7 cells, Ki = 0.16 μM. 17599916
COS7 Function assay Antagonist activity at human CXCR4 F172A mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover, Ki = 0.17 μM. 17599916
HEK293 Function assay Inhibition of Mab 12G5 binding to CXCR4 V280A mutant expressed in HEK293 cells, IC50 = 0.1753 μM. 19451305
COS7 Function assay Antagonist activity at human CXCR4 H281A mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover, Ki = 0.19 μM. 17599916
HEK293 Function assay Inhibition of Mab 12G5 binding to CXCR4 V112A mutant expressed in HEK293 cells, IC50 = 0.1966 μM. 19451305
COS7 Function assay Antagonist activity at human wild type CXCR4 expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover, Ki = 0.22 μM. 17599916
HEK293 Function assay Inhibition of Mab 12G5 binding to CXCR4 E275A mutant expressed in HEK293 cells, IC50 = 0.2356 μM. 19451305
CEM Function assay Displacement of [125I]CXCL12 from CXCR4 in human CEM cells, IC50 = 0.245 μM. 19053768
HEK293 Function assay Inhibition of Mab 12G5 binding to CXCR4 V99A mutant expressed in HEK293 cells, IC50 = 0.2585 μM. 19451305
HEK293 Function assay Inhibition of Mab 12G5 binding to CXCR4 H203A mutant expressed in HEK293 cells, IC50 = 0.259 μM. 19451305
HEK293 Function assay Inhibition of Mab 12G5 binding to CXCR4 I284A mutant expressed in HEK293 cells, IC50 = 0.2658 μM. 19451305
HEK293 Function assay Inhibition of Mab 12G5 binding to wild type CXCR4 expressed in HEK293 cells, IC50 = 0.2891 μM. 19451305
COS7 Function assay Antagonist activity at human CXCR4 H203A mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover, Ki = 0.29 μM. 17599916
COS7 Function assay Antagonist activity at transmembrane domain 6 of human CXCR4 I259A mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover, Ki = 0.29 μM. 17599916
COS7 Function assay Antagonist activity at human CXCR4 T287A mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover, Ki = 0.29 μM. 17599916
HEK293 Function assay Inhibition of Mab 12G5 binding to CXCR4 H113A mutant expressed in HEK293 cells, IC50 = 0.2964 μM. 19451305
HEK293 Function assay Inhibition of Mab 12G5 binding to CXCR4 W283A mutant expressed in HEK293 cells, IC50 = 0.3002 μM. 19451305
CEM-SS Antiviral assay Antiviral activity against HIV1 LAI in human CEM-SS cells assessed as inhibition of viral replication, IC50 = 0.32 μM. 19356827
COS7 Function assay Antagonist activity at human CXCR4 L120F mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover, Ki = 0.33 μM. 17599916
COS7 Function assay Antagonist activity at human CXCR4 Q200W mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover, Ki = 0.4 μM. 17599916
MT4 Antiviral assay Antiviral activity against HIV1 3B in human MT4 cells assessed as inhibition of viral replication, IC50 = 0.41 μM. 19356827
HEK293 Function assay Inhibition of Mab 12G5 binding to CXCR4 E277A mutant expressed in HEK293 cells, IC50 = 0.4695 μM. 19451305
COS7 Function assay Displacement of [125I]12G5 antibody from transmembrane domain 5 of human CXCR4 Q200A mutant expressed in COS7 cells, Ki = 0.56 μM. 17599916
HEK293 Function assay Inhibition of Mab 12G5 binding to CXCR4 H281A mutant expressed in HEK293 cells, IC90 = 0.5722 μM. 19451305
COS7 Function assay Antagonist activity at human CXCR4 I259W mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover, Ki = 0.63 μM. 17599916
COS7 Function assay Antagonist activity at human CXCR4 Y255A mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover, Ki = 0.66 μM. 17599916
COS7 Function assay Antagonist activity at human CXCR4 H113A mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover, Ki = 0.74 μM. 17599916
HEK293 Function assay Inhibition of Mab 12G5 binding to CXCR4 D181A mutant expressed in HEK293 cells, IC90 = 0.7956 μM. 19451305
HEK293 Function assay Inhibition of Mab 12G5 binding to CXCR4 V280A mutant expressed in HEK293 cells, IC90 = 0.8212 μM. 19451305
HEK293 Function assay Inhibition of Mab 12G5 binding to CXCR4 V112A mutant expressed in HEK293 cells, IC90 = 0.8213 μM. 19451305
HEK293 Function assay Inhibition of Mab 12G5 binding to CXCR4 H203A mutant expressed in HEK293 cells, IC90 = 0.8606 μM. 19451305
COS7 Function assay Displacement of [125I]12G5 antibody from human wild type CXCR4 expressed in COS7 cells, Ki = 0.89 μM. 17599916
COS7 Function assay Antagonist activity at human CXCR4 Q200A mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover, Ki = 0.93 μM. 17599916
HEK293 Function assay Inhibition of Mab 12G5 binding to CXCR4 E275A mutant expressed in HEK293 cells, IC90 = 0.9302 μM. 19451305
HEK293 Function assay Inhibition of Mab 12G5 binding to wild type CXCR4 expressed in HEK293 cells, IC90 = 0.9711 μM. 19451305
COS7 Function assay Displacement of [125I]12G5 antibody from transmembrane domain 7 of human CXCR4 I284A mutant expressed in COS7 cells, Ki = 1.1 μM. 17599916
COS7 Function assay Antagonist activity at human CXCR4 I284A mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover, Ki = 1.2 μM. 17599916
COS7 Function assay Displacement of [125I]12G5 antibody from transmembrane domain 6 of human CXCR4 I259A mutant expressed in COS7 cells, Ki = 1.5 μM. 17599916
COS7 Function assay Displacement of [125I]12G5 antibody from transmembrane domain 5 of human CXCR4 H203A mutant expressed in COS7 cells, Ki = 1.8 μM. 17599916
COS7 Function assay Antagonist activity at human CXCR4 D171N mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover, Ki = 1.8 μM. 17599916
COS7 Function assay Displacement of [125I]12G5 antibody from transmembrane domain 3 of human CXCR4 H113A mutant expressed in COS7 cells, Ki = 2 μM. 17599916
U87.CD4 Antiviral assay Antiviral activity against HIV1 clinical isolate 10 infected in U87.CD4 cells expressing human CXCR4 D262N mutant, IC50 = 2.541 μM. 17599916
U87.CD4 Antiviral assay Antiviral activity against HIV1 clinical isolate 10 infected in U87.CD4 cells expressing human CXCR4 D171ND262N mutant, IC50 = 2.694 μM. 17599916
COS7 Function assay Displacement of [125I]12G5 antibody from transmembrane domain 5 of human CXCR4 Q200W mutant expressed in COS7 cells, Ki = 2.7 μM. 17599916
COS7 Function assay Displacement of [125I]12G5 antibody from transmembrane domain 5 of human CXCR4 G207F mutant expressed in COS7 cells, Ki = 2.7 μM. 17599916
COS7 Function assay Displacement of [125I]12G5 antibody from transmembrane domain 5 of human CXCR4 G207W mutant expressed in COS7 cells, Ki = 3 μM. 17599916
COS7 Function assay Displacement of [125I]12G5 antibody from transmembrane domain 7 of human CXCR4 T287A mutant expressed in COS7 cells, Ki = 3.1 μM. 17599916
COS7 Function assay Displacement of [125I]12G5 antibody from transmembrane domain 4 of human CXCR4 F174A mutant expressed in COS7 cells, Ki = 3.2 μM. 17599916
COS7 Function assay Displacement of [125I]12G5 antibody from extracellular loop 2 of human CXCR4 D182A mutant expressed in COS7 cells, Ki = 3.2 μM. 17599916
COS7 Function assay Displacement of [125I]12G5 antibody from transmembrane domain 6 of human CXCR4 Y256A mutant expressed in COS7 cells, Ki = 4 μM. 17599916
COS7 Function assay Displacement of [125I]12G5 antibody from extracellular loop 2 of human CXCR4 N176A mutant expressed in COS7 cells, Ki = 4.1 μM. 17599916
COS7 Function assay Displacement of [125I]12G5 antibody from transmembrane domain 5 of human CXCR4 V196A mutant expressed in COS7 cells, Ki = 4.6 μM. 17599916
COS7 Function assay Displacement of [125I]12G5 antibody from transmembrane domain 6 of human CXCR4 I259W mutant expressed in COS7 cells, Ki = 4.6 μM. 17599916
COS7 Function assay Displacement of [125I]12G5 antibody from transmembrane domain 4 of human CXCR4 F172A mutant expressed in COS7 cells, Ki = 4.7 μM. 17599916
COS7 Function assay Antagonist activity at human CXCR4 D262N mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover, Ki = 4.7 μM. 17599916
COS7 Function assay Displacement of [125I]12G5 antibody from transmembrane domain 6 of human CXCR4 S263A mutant expressed in COS7 cells, Ki = 5.4 μM. 17599916
COS7 Function assay Antagonist activity at human CXCR4 E288A mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover, Ki = 6.4 μM. 17599916
MT4 Cytotoxicity assay Cytotoxicity against human MT4 cells by MTT assay, CC50 = 6.5 μM. 19356827
COS7 Function assay Antagonist activity at human CXCR4 A175F mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover, Ki = 8.5 μM. 17599916
COS7 Function assay Displacement of [125I]12G5 antibody from transmembrane domain 6 of human CXCR4 Y255A mutant expressed in COS7 cells, Ki = 9.7 μM. 17599916
MT-4 Function assay Concentration required to inhibit syncytia formation by 50% on HIV-1 infected MT-4 cells, EC50 = 10 μM. 9925728
COS7 Function assay Displacement of [125I]12G5 antibody from transmembrane domain 4 of human CXCR4 D171N mutant expressed in COS7 cells, Ki = 13 μM. 17599916
COS7 Function assay Displacement of [125I]12G5 antibody from extracellular loop 2 of human CXCR4 D187A mutant expressed in COS7 cells, Ki = 14 μM. 17599916
HL60 Function assay Displacement of [125I]SDF1alpha from CXCR4 in human HL60 cells, IC50 = 15.2 μM. 19188071
COS7 Function assay Displacement of [125I]12G5 antibody from extracellular loop 2 of human CXCR4 A175F mutant expressed in COS7 cells, Ki = 36 μM. 17599916
COS7 Function assay Displacement of [125I]12G5 antibody from transmembrane domain 6 of human CXCR4 D262N mutant expressed in COS7 cells, Ki = 46 μM. 17599916
COS, TZM-bl Function assay Inhibition of HIV1 NL4-3 envelope glycoprotein 120-mediated membrane fusion between virus-transfected african green monkey COS cells and human TZM-bl cells by luciferase-based cell-cell fusion assay in presence of IC9564 17954689
CXCR4+/CD4+/U87 Function assay Inhibition of HIV1 92TH594 infected CXCR4+/CD4+/U87 cells to assess co-receptor tropism as luciferase activity 17116663
CXCR4+/CD4+/U87 Function assay Inhibition of HIV1 HXB2 infected CXCR4+/CD4+/U87 cells to assess co-receptor tropism as luciferase activity 17116663
CHOK1 Function assay Induction of [125I]MCP1 dissociation from CCR2/CXCR4 expressed in CHOK1 cells by non-equilibrium binding assay 17715128
CHOK1 Function assay Antagonist activity at CXCR4 expressed in CHOK1 cells assessed as inhibition of SDF1-alpha-induced signaling by aequorin-based assay 17715128
CHOK1 Function assay Antagonist activity at CCR2/CXCR4 expressed in CHOK1 cells assessed as inhibition of SDF1-alpha-induced signaling by aequorin-based assay 17715128
CHOK1 Function assay Induction of [125I]SDF1alpha dissociation from CXCR4 expressed in CHOK1 cells by non-equilibrium binding assay 17715128
U87.CD4 Function assay Antagonist activity at human CXCR4 H281A mutant expressed in U87.CD4 cells assessed as inhibition of CXCL12-induced calcium mobilization 17599916
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生物活性

產(chǎn)品描述 Plerixafor (AMD3100, JM 3100, SID791)是一種趨化因子受體拮抗劑，作用于CXCR4和CXCL12介導(dǎo)的趨化性，無細(xì)胞試驗(yàn)中IC50分別為44 nM和5.7 nM。Plerixafor 可抑制human immunodeficiency virus (HIV)復(fù)制。
靶點(diǎn)
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抑制CXCL12介導(dǎo)的趨藥性，效能稍微高于其對CXCR4的親和力。[1]

Plerixafor也會拮抗SDF-1/CXCL12配體結(jié)合，IC50 為651 nM。Plerixafor抑制SDF-1介導(dǎo)的GTP-結(jié)合，SDF-1介導(dǎo)的鈣離子流和SDF-1刺激的趨藥性，IC50 分別為27 nM，572 nM 和51 nM。用它們的同源配體刺激時，Plerixafor不抑制表達(dá)CXCR3，CCR1，CCR2b，CCR4，CCR5或者CCR7的細(xì)胞中鈣離子流，Plerixafor也不會抑制LTB4的受體結(jié)合。Plerixafor自身不會在表達(dá)多重GPCRs ，包括CXCR4，CCR4和CCR7的CCRF–CEM細(xì)胞中誘導(dǎo)鈣離子流。[2]
實(shí)驗(yàn)圖片 檢測方法 檢測指標(biāo) 實(shí)驗(yàn)圖片 PMID
Immunofluorescence CXCR4 β-arrestin2 28521261
體內(nèi)研究(In Vivo)
體內(nèi)研究活性

在糖尿病小鼠體內(nèi)，Plerixafor單劑量局部給藥促進(jìn)傷口愈合，通過增加細(xì)胞因子產(chǎn)生，動員骨髓EPCs，并增強(qiáng)成纖維細(xì)胞和單核細(xì)胞/巨噬細(xì)胞，從而增加血管新生和血管生成發(fā)揮作用。[3]

同類小鼠以PBS，IGF1，PDGF，SCF，或VEGF連續(xù)給藥5天，在第5天給藥Plerixafor。與PDGF，SCF和VEGF結(jié)合Plerixafor的試驗(yàn)組相比，IGF1加Plerixafor的注射小鼠中，菌落的數(shù)量和大小最高。[4]
動物實(shí)驗(yàn) Animal Models 節(jié)段性骨缺損的12周大C57BL/6小鼠
Dosages 5 mg/kg
Administration i.p.
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|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 502.78 分子式

C28H54N8
CAS號 110078-46-1 SDF Download Plerixafor (AMD3100) SDF
Smiles C1CNCCNCCCN(CCNC1)CC2=CC=C(C=C2)CN3CCCNCCNCCCNCC3
儲存條件(自收到貨起)

體外溶解度
批次：

Ethanol : 100 mg/mL (198.89 mM)

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

Water : 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(shí)驗(yàn)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(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)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(jìn)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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常見問題及建議解決方法

問題 1:
How about the half-life of the product (Cat S8030)?

回答：
The biological half-life for this drug is 3-5 hours: https://en.wikipedia.org/wiki/Plerixafor.

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