Plerixafor (AMD3100)

Catalog No.S8030 Synonyms: JM 3100, SID791

For research use only.

Plerixafor (AMD3100, JM 3100, SID791) is a chemokine receptor antagonist for CXCR4 and CXCL12-mediated chemotaxis with IC50 of 44 nM and 5.7 nM in cell-free assays, respectively. Plerixafor inhibits human immunodeficiency virus (HIV) replication.

Plerixafor (AMD3100) Chemical Structure

CAS No. 110078-46-1

Selleck's Plerixafor (AMD3100) has been cited by 81 publications

Purity & Quality Control

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Biological Activity

Description Plerixafor (AMD3100, JM 3100, SID791) is a chemokine receptor antagonist for CXCR4 and CXCL12-mediated chemotaxis with IC50 of 44 nM and 5.7 nM in cell-free assays, respectively. Plerixafor inhibits human immunodeficiency virus (HIV) replication.
Targets
CXCL12 [1]
(Cell-free assay)
CXCR4 [1]
(Cell-free assay)
5.7 nM 44 nM
In vitro

Plerixafor inhibits CXCL12-mediated chemotaxis with a potency lightly better than its affinity for CXCR4. [1] Plerixafor also antagonizes SDF-1/CXCL12 ligand binding with an IC50 of 651 nM. Plerixafor inhibits SDF-1 mediated GTP-binding, SDF-1 mediated calcium flux and SDF-1 stimulated chemotaxis with IC50 of 27 nM, 572 nM and 51 nM, respectively. Plerixafor does not inhibit calcium flux against cells expressing CXCR3, CCR1, CCR2b, CCR4, CCR5 or CCR7 when stimulated with their cognate ligands, nor does Plerixafor inhibit receptor binding of LTB4. Plerixafor does not, on its own, induce a calcium flux in the CCRF–CEM cells, which express multiple GPCRs including CXCR4, CCR4 and CCR7. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
CHOK1 NIjvNWNHfW6ldHnvckBie3OjeR?= MXjEbZNxdGGlZX3lcpQhd2ZiW{GyOWleW0SIMXHsdIhiKG[{b32gR2NTOi:FWFPSOEBmgHC{ZYPz[YQhcW5iQ1jPT|Eh[2WubIOsJGlEPTBiPTCwMlAxODB2IN88UU4> MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzdzNUGyPEc,OTd5MUWxNlg9N2F-
CHOK1 NYnLWXU4TnWwY4Tpc44h[XO|YYm= Mn\pSIl{eGyjY3Xt[Y51KG:oIGuxNlVKZU2FUEGg[pJwdSCFQ2KyM2NZS1J2IHX4dJJme3OnZDDpckBEUE:NMTDj[YxteyxiSVO1NEA:KDBwMECwNFkh|ryPLh?= NFPHUm09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{exOVEzQCd-MUe3NVUyOjh:L3G+
CHOK1 NFzkVYhHfW6ldHnvckBie3OjeR?= NETTc4xFcXOybHHj[Y1mdnRib3[gX|EzPUmfU1TGNYFteGijIH\yc40hS1iFUkSg[ZhxemW|c3XkJIlvKEOKT1uxJINmdGy|LDDJR|UxKD1iMD6wNFA5OSEQvF2u MnPQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd5MUWxNlgoRjF5N{G1NVI5RC:jPh?=
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MT-4 M{X0eWZ2dmO2aX;uJIF{e2G7 M3\OeGVn\mWldHn2[UBkd26lZX70doF1cW:wIHHnZYlve3RiSFnWMVIpWk:GKTDy[ZBtcWOjdHnvckBqdiCPVD20JINmdGy|LDDFR|UxKD1iMD6wNFU6KM7:TT6= NWPXT4hxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxOEW2PFc6Pyd-OEW2PFc6PzxxYU6=
CEM-CCRF NFfqdnFHfW6ldHnvckBie3OjeR?= MUezNEBucW6| NVXrR2RXUW6qaXLpeIlwdiCxZjDQSU1kd26sdXfheIVlNTF{R{WgZY51cS2FWFPSOEBidnSrYn;kfUBjcW6maX7nJJRwKEO[Q2K0JIlvKGi3bXHuJGNGVS2FQ2LGJINmdGy|IIDy[Ylv[3WkYYTl[EBnd3JiM{CgcYlveyCob3zsc5dm\CCkeTDhcpRq[m:meTDh[IRqfGmxbjDifUBHSUOVIFPhcpRwKEmLIHP5eI9ndHWxcn;t[ZRzcWNiYX7hcJl{cXNuIFnDOVAhRSByLkCwOkDPxE1w MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzV5MUCzPEc,Ojd3N{GwN|g9N2F-
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Assay
Methods Test Index PMID
Immunofluorescence CXCR4 ; β-arrestin2 28521261 31186083
In vivo A single topical application of Plerixafor promotes wound healing in diabetic mice by increasing cytokine production, mobilizing bone marrow EPCs, and enhancing the activity of fibroblasts and monocytes/macrophages, thereby increasing both angiogenesis and vasculogenesis. [3] Cohorts of mice are administered with PBS, IGF1, PDGF, SCF, or VEGF for five consecutive days and Plerixafor on the 5th day. The number and size of the colonies are highest in IGF1 plus Plerixafor injected mice compared to PDGF, SCF and VEGF treated groups, in combination with Plerixafor. [4]

Protocol (from reference)

Animal Research:[4]
  • Animal Models: Twelve-week-old C57BL/6 mice with segmental bone defect
  • Dosages: 5 mg/kg
  • Administration: Administered via i.p.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 502.78
Formula

C28H54N8

CAS No. 110078-46-1
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CNCCNCCCN(CCNC1)CC2=CC=C(C=C2)CN3CCCNCCNCCCNCC3

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05421416 Not yet recruiting Drug: Loratadine|Drug: Placebo Stem Cell Transplant Complications AHS Cancer Control Alberta November 1 2022 Phase 2
NCT05343572 Not yet recruiting Drug: Plerixafor Asherman Syndrome|Atrophic Endometrium|Recurrent Implantation Failure Hugh Taylor|Yale University September 2022 Early Phase 1
NCT05411575 Recruiting Drug: Plerixafor 20 MG/ML [Mozobil]|Other: Placebo COVID-19 Acute Respiratory Distress Syndrome|COVID-19 4Living Biotech|4P-Pharma July 19 2022 Phase 2
NCT05445128 Recruiting Biological: MGTA-145|Drug: Plerixafor Sickle Cell Disease Magenta Therapeutics Inc.|bluebird bio June 24 2022 Phase 2
NCT04646603 Recruiting Drug: MRG-001|Drug: Placebo COVID-19|ARDS Human|Stem Cells|Regeneration MedRegen LLC|ICON plc|Johns Hopkins University December 1 2021 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-08-01)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Frequently Asked Questions

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

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

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