239825
AMD3100
≥98% (HPLC), CXCR4 receptor antagonist, liquid
别名:
InSolution CXCR4 Antagonist I, AMD3100, 1,1ʹ(1,4-Phenylenebis(methylene))-bis-1,4,8,11-tetraazacyclotetradecane, 8HCl, 4H₂O, 1,4-bis((1,4,8,11-Tetraazacyclotetradecan-1-yl)methyl)benzene, 8HCl, 4H₂O
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关于此项目
经验公式（希尔记法）:
C28H54N8 · 8HCl · 4H2O
化学文摘社编号:
分子量:
866.53
MDL number:
UNSPSC Code:
51111800
NACRES:
NA.77
产品名称
AMD3100, InSolution, ≥98%, 50 mM aqueous solution, CXCR4 antagonist I
SMILES string
Cl.Cl.Cl.Cl.Cl.Cl.Cl.Cl.N3(CCNCCCNCCNCCC3)Cc1ccc(cc1)CN2CCNCCCNCCNCCC2
InChI
1S/C28H54N8.8ClH/c1-9-29-15-17-31-13-3-21-35(23-19-33-11-1)25-27-5-7-28(8-6-27)26-36-22-4-14-32-18-16-30-10-2-12-34-20-24-36;;;;;;;;/h5-8,29-34H,1-4,9-26H2;8*1H
InChI key
UEUPDYPUTTUXLJ-UHFFFAOYSA-N
assay
≥98% (HPLC)
form
liquid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
avoid repeated freeze/thaw cycles
protect from light
shipped in
dry ice
storage temp.
−70°C
Quality Level
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Preparation Note
Following initial thaw, aliquot and freeze (-70°C). Aliquots are stable for up to 1 year at -70°C.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
CXCR4
CXCR4
Reversible: yes
Disclaimer
Toxicity: Standard Handling (A)
General description
A symmetrical bicyclam compound that antagonizes CXCL12 (SDF1) binding to CXCR4 (IC50 = 108 and 245 nM using rat and human CXCR4, respectively) and inhibits SDF1-induced Ca2+ flux (by 100% at 100 ng/ml in SUP-T1 and THP-1 cultures) as well as CXCR4-, but not CCR5-, mediated HIV infection (IC50 = 200 nM), while enhancing the binding of SDF1 to CXCR7 (by ~60% at 1 mM with CXCR7-expressing HEK293T cells) and SDF1-induced β-arrestin recruitment to CXCR7 (EC50 = 6.48 and 11.8 nM, in the presence and absence of 10 µM AMD3100, respectively). Administration AMD3100 via intravenous infusion is also reported to result in hematopoietic stem cell mobilization in humans, dogs, and mice in vivo. Exhibits no inhibitory effects against chemokine-induced signaling via CXCR1/2/3 or CCR1/2/3/4/5/6/7/8/9.
Other Notes
Kalatskaya, I., et al. 2009. Mol. Pharmacol.77, 1240.
Pitchford, S.C., et al. 2009. Cell Stem Cell4, 62.
De Clercq, E. 2009. Biochem. Pharmacol.77, 1655.
Thoma, G., et al. 2008. J. Med. Chem.51, 7915.
De Clercq, E. 2000. Mol. Pharmacol.57, 833.
Pitchford, S.C., et al. 2009. Cell Stem Cell4, 62.
De Clercq, E. 2009. Biochem. Pharmacol.77, 1655.
Thoma, G., et al. 2008. J. Med. Chem.51, 7915.
De Clercq, E. 2000. Mol. Pharmacol.57, 833.
Packaging
Packaged under inert gas
Physical form
A 50 mM (15 mg/308 µL) solution of CXCR4 Antagonist I, AMD3100 (Cat. No. 239820) in H₂O.
存储类别
10 - Combustible liquids
wgk
WGK 3
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