Plerixafor octahydrochloride (JM3100 octahydrochloride) blocks the binding of stromal cell-derived factor (SDF-1alpha) to the cellular receptor CXCR4, resulting in hematopoietic stem cell (HSC) release from bone marrow and HSC movement into the peripheral circulation. Plerixafor is a bicyclam with hematopoietic stem cell-mobilizing activity.

CXCL12:5.7 nM, CXCR4:44 nM

AMD 3100 能抑制初代T4淋巴细胞中低通道临床HIV-1分离株（K31、D370、K6/-2、HEM和JRCSF）的复制（EC50s：0.16-1.5 ng/ml；EC90s：0.36-4.7 ng/ml）。在初代单核细胞中，AMD 3100 对HIV-1（K31和SF-162）具有活性，其EC50s为0.28-7.2 ng/mL，EC90s为0.68-12 ng/mL。

在通过皮下途径给予兔子AMD 3100（10 mg/kg）后，其血清中化合物浓度是通过基于该化合物对MT-4细胞中HIV-1细胞毒性抑制所需EC50的生物检测方法来确定的。

Plerixafor is dissolved in DMSO and then diluted with appropriate medium[2]. U87 mg cells are seeded in 96-well plates at the density of 6×103 cells in 200 μL/well and treated with CXCL12, Plerixafor or with peptide R, as described in the previous "Treatments" section. MTT (5 μg/mL) is added at each time point (24, 48, 72 h) during the final 2 h of treatment. After removing cell medium, 100 μL DMSO are added and optical densities measured at 595 nm with a LT-4000MS Microplate Reader. Measurements are made in triplicates from three independent experiments[2].