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CXCR4 Antagonist I, AMD3100
1,1′-(1,4-Phenylenebis(methylene))-bis-1,4,8,11-tetraazacyclotetradecane, 8HCl, JM3100
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. Also available as a 50 mM solution in H2O (Cat. No. 239825).
产品信息
Form Off-white solid
Molar mass 794.5
Protect from Light 是的
Hygrocopic 是的
Packaged under inert gas 是的
Purity ≥98% by HPLC
Solubility H2O
Chemical formula C28H54N8 • 8HCl
CAS number 155148-31-5
商店和运输信息
Storage +2°C to +8°C
Ship Ambient Temperature Only
Standard Handling |