|1,4-双((1,4,8,11-四氮杂环十四烷-1-基)甲基)苯八盐酸盐|CsnPharm

CAS No.: 155148-31-5

Plerixafor octaHCl/盐酸普乐沙福 Catalog No. CSN16151

Synonyms: AMD3100 octahydrochloride;JM3100 octahydrochloride;SID791 octahydrochloride

Plerixafor 8HCl is a chemokine receptor antagonist for CXCR4 and CXCL12-mediated chemotaxis with IC50 of 44 nM and 5.7 nM, respectively.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 CXCL12

IC50:5.7nM CXCR4

IC50:44nM
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 inflammation or infection sites and implicated in several immuno-related disease states, organogenesis, angiogenesis and tumor growth and metastasis. Plerixafor Octahydrochloride is the hydrochloride form of AMD3100. 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
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
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

更多
动物研究
剂量
Mice^[3]: 0.625 mg/kg - 10 mg/kg (s.c.) Rat^[3]: 25 mg/kg (s.c.), 2 mg/kg (i.v.)

给药途径
s.c., i.v.

动物研究
剂量	Mice^[3]: 0.625 mg/kg - 10 mg/kg (s.c.) Rat^[3]: 25 mg/kg (s.c.), 2 mg/kg (i.v.)
给药途径	s.c., i.v.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.2587 mL
- 6.2935 mL
- 12.5870 mL
- 5 mM
- 0.2517 mL
- 1.2587 mL
- 2.5174 mL
- 10 mM
- 0.1259 mL
- 0.6294 mL
- 1.2587 mL

技术信息

CAS号

155148-31-5

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C28H62Cl8N8

运输

蓝冰

分子量

794.47

别名

AMD3100 octahydrochloride;JM3100 octahydrochloride;SID791 octahydrochloride;AMD3100 8HCl;JM-3100 8HCl;SID 791 8HCl;AMD-3100;JM-3100;SDZ-SID-791;JLK-169;SID-791;JM-2987;Plerixafor HCl;MOZOBIL;盐酸普乐沙福

溶解度

DMSO	insoluble warming
Water	95.0 mg/mL (119.6 mM)

动物实验配方

0.5% CMC-Na

80 mg/mL

suspension

大规格询价

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Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources

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
human HL60 cells	-	Function assay	-	Displacement of [125I]SDF1alpha from CXCR4 in human HL60 cells, IC50=15.2 μM	19188071
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
human MOLT4 cells	1000 nM	Function assay	-	Inhibition of Mab 12G5 binding to CXCR4 expressed in human MOLT4 cells at 1000 nM by FACS analysis	19451305
human MT2 cells	1 ug/mL	Function assay	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 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
human U87 cells	1000 nM	Function assay	-	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
MT-4 cells	-	Function assay	-	Effective concentration of compound against HIV-1 IIIB strain in MT-4 cells, EC50=65 nM	14698189
PBMC cells	-	Function assay	-	Effective concentration of compound against HIV-1 89.6 strain in PBMC cells, EC50=3.8 nM	14698189
rat IR983F cells	-	Function assay	-	Displacement of [125I]CXCL12 from CXCR4 in rat IR983F cells, IC50=108 nM	19053768

靶点	Description	IC50
CXCL12		IC50:5.7nM
CXCR4		IC50:44nM

Plerixafor octaHCl/盐酸普乐沙福 Catalog No. CSN16151

靶点选择性

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