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Plerixafor (AMD3100) 8HCl CXCR Antagonist

Name: Plerixafor (AMD3100) 8HCl
Brand: Selleck Chemicals
SKU: S3013
Rating: 5 (52 reviews)

Cat.nr.: S3013

Plerixafor (AMD3100, JM 3100, Plerixafor Octahydrochloride, AMD3100 octahydrochloride, SID791 octahydrochloride) 8HCl is het hydrochloride van Plerixafor, een chemokine receptor antagonist voor CXCR4 en CXCL12-gemedieerde chemotaxis met IC50 van respectievelijk 44 nM en 5,7 nM in celvrije assays. Plerixafor kan worden gebruikt als een anti-HIV middel.

Plerixafor (AMD3100) 8HCl CXCR Antagonist Chemical Structure

Chemische structuur

Molecuulgewicht: 794.47

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Kwaliteitscontrole (Quality Control)

Batch: Zuiverheid: 99.90%

99.90

Gerelateerde doelwitten	Hedgehog/Smoothened PKA Adrenergic Receptor AChR 5-HT Receptor Histamine Receptor Dopamine Receptor Ras KRas GPR
Overig CXCR Inhibitoren	AZD5069 SB 225002 Reparixin (Repertaxin) WZ811 Navarixin (SCH-527123) LIT-927 SX-682 AMG 487 SB 265610 LY2510924

Celkweek, behandeling & werkzame concentratie
(Cell Culture, Treatment & Working Concentration)

Cellijnen	Assaytype	Concentratie	Incubatietijd	Activiteitsbeschrijving	PMID
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
PBMC cells	Function assay			Effective concentration of compound against HIV-1 89.6 strain in PBMC cells, EC50=3.8 nM	14698189
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 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
MT-4 cells	Function assay			Effective concentration of compound against HIV-1 IIIB strain in MT-4 cells, EC50=65 nM	14698189
rat IR983F cells	Function assay			Displacement of [125I]CXCL12 from CXCR4 in rat IR983F cells, IC50=108 nM	19053768
CEM-SS cells	Function assay			Effective concentration of compound against HIV-1 LAI strain in CEM-SS cells, EC50=127 nM	14698189
human HL60 cells	Function assay			Displacement of [125I]SDF1alpha from CXCR4 in human HL60 cells, IC50=15.2 μM	19188071
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 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 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
MT4	Antiviral assay			Antiviral activity against HIV1 3B assessed as reduction in cytopathic effect in MT4 cells, EC50=0.011μM	17034122
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			Antiviral activity against X4-tropic HIV1 NL4.3 infected in human MT4 cells assessed as protection from virus-induced cytopathogenicity, EC50=0.062μM	22579418
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
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
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
Klik om meer experimentele gegevens over cellijnen te bekijken

Chemische informatie, opslag en stabiliteit (Chemical Information, Storage & Stability)

Molecuulgewicht	794.47	Formule	C₂₈H₅₄N₈.8HCl	Opslag (vanaf de datum van ontvangst)	3 jaar-20°Cpoeder
CAS-nr.	155148-31-5	SDF downloaden		Opslag van stamoplossingen	1 jaar-80°Cin oplosmiddel 1 maand-20°Cin oplosmiddel
Synoniemen	JM 3100 8HCl,Plerixafor Octahydrochloride,AMD3100 octahydrochloride,SID791 octahydrochloride			Smiles	C1CNCCNCCCN(CCNC1)CC2=CC=C(C=C2)CN3CCCNCCNCCCNCC3.Cl.Cl.Cl.Cl.Cl.Cl.Cl.Cl

Oplosbaarheid (Solubility)

In vitro
Batch:

Water : 100 mg/mL

DMSO : Insoluble
(Met vocht verontreinigd DMSO kan de oplosbaarheid verminderen. Gebruik verse, watervrije DMSO.)

Ethanol : Insoluble

Molariteitscalculator

Massa	Concentratie	Volume	Molecuulgewicht
=	×	×

Verdunningscalculator Molecuulgewichtcalculator

In vivo Batch:
Clear solution	Saline Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	30.000mg/ml (37.76mM)	Taking the 1 mL working solution as an example, add 30 mg of this product to 1 ml of physiological saline (0.9% NaCL solution), mix evenly to make it clear, The mixed solution should be used immediately for optimal results.

In vivo formulatiecalculator (heldere oplossing)

Stap 1: Voer onderstaande informatie in (Aanbevolen: een extra dier om rekening te houden met verlies tijdens het experiment)

Dosering: mg/kg Gemiddeld gewicht van dieren: g Doseervolume per dier:μL Aantal dieren:

Stap 2: Voer de in vivo formulering in (Dit is alleen de calculator, geen formulering. Neem eerst contact met ons op als er geen in vivo formulering is in de sectie oplosbaarheid.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Berekeningsresultaten:

Werkconcentratie: mg/ml;

Methode voor het bereiden van DMSO-moedervloeistof: mg geneesmiddel vooropgelost in μL DMSO ( Concentratie moedervloeistof mg/mL, Neem eerst contact met ons op als de concentratie de DMSO-oplosbaarheid van de batch van het geneesmiddel overschrijdt. )

Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toeμL PEG300, mengen en verhelderen, daarna toevoegenμL Tween 80, mengen en verhelderen, daarna toevoegen μL ddH₂O, mengen en verhelderen.

Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toe μL Maïsolie, mengen en verhelderen.

Opmerking: 1. Zorg ervoor dat de vloeistof helder is voordat u het volgende oplosmiddel toevoegt.
2. Zorg ervoor dat u het/de oplosmiddel(en) in de juiste volgorde toevoegt. U moet ervoor zorgen dat de verkregen oplossing, bij de vorige toevoeging, een heldere oplossing is voordat u verdergaat met het toevoegen van het volgende oplosmiddel. Fysieke methoden zoals vortexen, ultrasoon of een warmwaterbad kunnen worden gebruikt om het oplossen te bevorderen.

Werkingsmechanisme (Mechanism of Action)

Targets/IC₅₀/Ki	CXCL12 (Cell-free assay) 5.7 nM CXCR4 (Cell-free assay) 44 nM
In vitro	Plerixafor inhibits CXCL12-mediated chemotaxis with a potency lightly better than its affinity for CXCR4. 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.
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. 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.
Referenties	[1] https://pubmed.ncbi.nlm.nih.gov/19641136/ [2] https://pubmed.ncbi.nlm.nih.gov/16815309/ [3] https://pubmed.ncbi.nlm.nih.gov/22048734/ [4] https://pubmed.ncbi.nlm.nih.gov/22342795/

Toepassingen (Applications)

Methoden	Biomarkers	Afbeeldingen	PMID
Immunofluorescence	CXCR4 β-arrestin2		28521261

Informatie over klinische proeven (Clinical Trial Information)

(gegevens van https://clinicaltrials.gov, bijgewerkt op 2024-05-22)

NCT-nummer	Werving	Aandoeningen	Sponsor/medewerkers	Startdatum	Fasen
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	--

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