Plerixafor 8HCl (AMD3100 8HCl) Chemische Eigenschaften,Einsatz,Produktion Methoden
S-Sätze Betriebsanweisung:
S22:Staub nicht einatmen.
S24/25:Berührung mit den Augen und der Haut vermeiden.
Verwenden
Plerixafor 8HCl (AMD3100 8HCl) is the hydrochloride of Plerixafor, a chemokine receptor antagonist for CXCR4 and CXCL12-mediated chemotaxis with IC50 of 44 nM and 5.7 nM, respectively - See more at: http://www.selleckchem.com/products/plerixafor-8hcl-db06
Allgemeine Beschreibung
A symmetrical bicyclam compound that antagonizes CXCL12 (SDF1) binding to CXCR4 (IC
50 = 108 and 245 nM using rat and human CXCR4, respectively) and inhibits SDF1-induced Ca
2+ flux (by 100% at 100 ng/ml in SUP-T1 and THP-1 cultures) as well as CXCR4-, but not CCR5-, mediated HIV infection (IC
50 ≤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 (EC
50 = 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.
Biologische Aktivität
Highly selective CXCR4 chemokine receptor antagonist (IC 50 values are 0.02 - 0.13 and > 25 μ M for CXCR4 and all other chemokine receptors respectively). Switches inflammatory responses from Th2 to Th1 type and reduces airway hyperresponsiveness in a mouse model of asthma. Potently inhibits HIV-1 and HIV-2 replication in vitro (EC 50 = 4 - 35 nM) and mobilizes hematopoietic stem cells in vivo .
Clinical Use
Plerixafor hydrochloride, a chemokine CXCR4 (SDF-1) antagonist,
was launched by Genzyme for the treatment of enhancing
mobilization of hematopoietic stem cells for autologous transplantation
in patients with lymphoma and enhancing mobilization of
hematopoietic stem cells for transplantation in patients with multiple
myeloma. Being a CXCR4 antagonist, a specific cellular chemokine
receptor, plerixafor triggers the rapid movement of stem
cells out of the bone marrow and into circulating blood where
the stem cells can be collected for use in stem cell transplants.
Regarding its use for cardiac applications, some clinical data suggests
that the presence of stem cells circulating in the bloodstream
or directly injected into the hearts of patients who have suffered a
heart attack may result in improved cardiac function.
Plerixafor 8HCl (AMD3100 8HCl) Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
