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Plerixafor (AMD3100)

別名：JM 3100, SID791

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)化学構造

CAS No. 110078-46-1

サイズ 価格(税別) 在庫状況
JPY 22000 国内在庫あり
JPY 37000 国内在庫あり
JPY 85500 国内在庫あり
JPY 448500 国内在庫なし(納期7~10日)

代表番号: 045-509-1970|電子メール：sales@selleck.co.jp
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Plerixafor (AMD3100)関連製品

シグナル伝達経路

CXCR Signaling Pathways

CXCRシグナル伝達経路

CXCR阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
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
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生物活性

製品説明 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
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]
Kinase Assay Receptor binding assays
For the competition binding studies against CXCR4, a concentration range of Plerixafor is incubated for 3 hours at 4 °C in binding buffer (PBS containing 5 mM MgCl2, 1 mM Ca Cl2, 0.25% BSA, pH 7.4) with 5 × 105 CCRF–CEM cells and 100 pM 125I-SDF-1α (2200 Ci/mmol) in Milipore DuraporeTM filter plates. Unbound 125I-SDF-1α is removed by washing with cold 50 mM HEPES, 0.5 M NaCl pH 7.4. The competition binding assay against BLT1 is performed on membranes from CHO-S cells expressing recombinant BLT1. The membranes are prepared by mechanical cell lysis followed by high speed centrifugation, re-suspended in 50 mm HEPES, 5 mM MgCl2 buffer and flash frozen. The membrane preparation is incubated with Plerixafor for 1 hour at room temperature in an assay mixture containing 50 mM Tris, pH 7.4, 10 mM MgCl2, 10 mM CaCl2, 4 nM LTB4 mixed with 1 nM 3H-LTB4 (195.0 Ci/mmol) and 8 μg membrane. The unbound 3H-LTB4 is separated by filtration on Millipore Type GF-C filter plates.
実験結果図 Methods Biomarkers 結果図 PMID
Immunofluorescence β-arrestin2 CXCR4 31186083
In Vivo
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]
動物実験 動物モデル Twelve-week-old C57BL/6 mice with segmental bone defect
投与量 5 mg/kg
投与経路 Administered via 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 --

化学情報

分子量 502.78 化学式

C28H54N8
CAS No. 110078-46-1 SDF Download Plerixafor (AMD3100) SDFをダウンロードする
Smiles C1CNCCNCCCN(CCNC1)CC2=CC=C(C=C2)CN3CCCNCCNCCCNCC3
保管

In vitro
Batch:

Ethanol : 100 mg/mL

DMSO : Insoluble ( 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機
Clear solution
5%absolute ethyl alcohol 40% 5% 50%ddH2O
1.1mg/ml (2.19mM) Taking the 1 mL working solution as an example, add 50 μL of 22 mg/ml absolute ethyl alcohol stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

mg/kg g μL 匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH2O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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よくある質問（FAQ）

質問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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