Other grades of this product :
| CXCR4 Antagonist II - CAS 1258011-83-4 - Calbiochem Basic information |
| CXCR4 Antagonist II - CAS 1258011-83-4 - Calbiochem Chemical Properties |
| CXCR4 Antagonist II - CAS 1258011-83-4 - Calbiochem Usage And Synthesis |
| General Description | A thiopseudourea compound that acts as a selective and highly potent CXCR4/Fusin antagonist (IC50 = 1.1 nM against SDF-1/CXCL12-induced Ca2+ mobilization in CEM cells) and effectively targets CXCR4-mediated binding of both CXCL12 (IC50 = 8 and 11 nM in competitive binding assays using human CEM and rat IR983F membrane, respectively) and HIV gp120 (IC50 = 7 nM in HIV attachment assays). Shown to be orally available in rat with good in vivo pharmacokinetics (32% availability, tmax = 0.5 h, Cmax= 18 ng/ml, t1/2 = 7.6 h, based on an oral dose of 1 mg/kg). Comparing to AMD3100 (Cat. No. 239820), CXCR4 Antagonist II is ~30-times more potent as a CXCR4-CXCL12 interaction blocker, while being ~2-fold less potent in blocking gp120-mediated HIV attachment. |
| CXCR4 Antagonist II - CAS 1258011-83-4 - Calbiochem Preparation Products And Raw materials |
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