CXCR4 Antagonist II - CAS 1258011-83-4 - Calbiochem

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, t_max = 0.5 h, C_max= 18 ng/ml, t_1/2 = 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.