Home GPCR & G Protein CXCR 길항제 Plerixafor (AMD3100) 8HCl

연구용

Plerixafor (AMD3100) 8HCl CXCR 길항제

제품 번호: S3013

Plerixafor (AMD3100) 8HCl은 CXCR4 및 CXCL12 매개 화학주성(chemotaxis)에 대한 케모카인 수용체 길항제인 Plerixafor의 염산염으로, 세포가 없는 분석(cell-free assays)에서 각각 44 nM 및 5.7 nM의 IC50 값을 나타냅니다. Plerixafor는 항-HIV 제제로 사용될 수 있습니다.
Plerixafor (AMD3100) 8HCl CXCR 길항제 Chemical Structure

화학 구조

분자량: 794.47

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품질 관리 (Quality Control)

배치: 순도: 99.90%
99.90

세포 배양, 처리 및 작업 농도
(Cell Culture, Treatment & Working Concentration)

세포주 분석 유형 농도 배양 시간 제형 활성 설명 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
클릭하여 더 많은 세포주 실험 데이터 보기

화학 정보, 보관 및 안정성 (Chemical Information, Storage & Stability)

분자량 794.47 화학식

C28H54N8.8HCl

 보관 (수령일로부터)
CAS 번호 155148-31-5 SDF 다운로드 원액 보관

동의어 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

용해도 (Solubility)

In vitro
배치:

Water : 100 mg/mL

DMSO : Insoluble
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : Insoluble

몰농도 계산기

질량 농도 부피 분자량
희석 계산기 분자량 계산기

In vivo
배치:

생체 내 제형 계산기 (투명한 용액)

1단계: 아래 정보 입력 (권장: 실험 중 손실을 고려하여 추가 동물 포함)

mg/kg g μL

2단계: 생체 내 제형 입력 (이것은 계산기일 뿐 제형이 아닙니다. 용해도 섹션에 생체 내 제형이 없는 경우 먼저 당사에 문의하십시오.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

계산 결과:

작업 농도: mg/ml;

DMSO 원액 준비 방법: mg 약물 사전 용해 μL DMSO ( 원액 농도 mg/mL, 농도가 해당 약물 배치의 DMSO 용해도를 초과하는 경우 먼저 당사에 문의하십시오. )

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가μL PEG300, 혼합하고 투명하게 한 다음 추가μL Tween 80, 혼합하고 투명하게 한 다음 추가 μL ddH2O, 혼합하고 투명하게 합니다.

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가 μL 옥수수 기름, 혼합하고 투명하게 합니다.

참고: 1. 다음 용매를 추가하기 전에 액체가 투명한지 확인하십시오.
2. 용매를 순서대로 추가해야 합니다. 다음 용매를 추가하기 전에 이전 추가에서 얻은 용액이 투명한 용액인지 확인해야 합니다. 와동, 초음파 또는 뜨거운 물 중탕과 같은 물리적 방법을 사용하여 용해를 도울 수 있습니다.

작용 메커니즘 (Mechanism of Action)

Targets/IC50/Ki
CXCL12
(Cell-free assay)
5.7 nM
CXCR4
(Cell-free assay)
44 nM
시험관 내(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.

생체 내(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.

참조
  • [4] https://pubmed.ncbi.nlm.nih.gov/22342795/

적용 분야 (Applications)

방법 바이오마커 이미지 PMID
Immunofluorescence CXCR4 β-arrestin2
S3013-IF1
28521261

임상시험 정보 (Clinical Trial Information)

(데이터 출처 https://clinicaltrials.gov, 업데이트 날짜 2024-05-22)

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NCT05844527 Recruiting
Wound of Skin|Abdominal Wound
MedRegen LLC
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COVID-19 Acute Respiratory Distress Syndrome|COVID-19
4Living Biotech|4P-Pharma
 July 19 2022 Phase 2
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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 --