239820
CXCR4 Antagonist I, AMD3100
1,1′-(1,4-Phenylenebis(methylene))-bis-1,4,8,11-tetraazacyclotetradecane, 8HCl, JM3100
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メルク株式会社
目黒区下目黒1-8-1
153-8927 東京
Japan
TEL： 0120-189-390
Fax: 0120-189-350
E-mail mj_service@merckgroup.com
31 5月 2012
ローディング
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.
| 製品情報 | |||
|---|---|---|---|
| Form | Off-white solid | ||
| Protect from Light | はい | ||
| Hygrocopic | はい | ||
| Packaged under inert gas | はい | ||
| Purity | ≥98% by HPLC | ||
| 化学式 | C28H54N8 • 8HCl | ||
| CAS 番号 | 155148-31-5 | ||
| 保管と送付情報 | |||
|---|---|---|---|
| Storage | +2°C to +8°C | ||
| Ship |
Ambient Temperature Only
Standard Handling |
||
