1. GPCR/G Protein
  2. CXCR

Plerixafor octahydrochloride (Synonyms: AMD3100 octahydrochloride; JM3100 octahydrochloride; SID791 octahydrochloride)

Cat. No.: HY-50912 Purity: 98.90%
Handling Instructions

Plerixafor octahydrochloride is a selective CXCR4 antagonist with IC50 of 44 nM.

For research use only. We do not sell to patients.
Plerixafor octahydrochloride Chemical Structure

Plerixafor octahydrochloride Chemical Structure

CAS No. : 155148-31-5

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Customer Review

Other Forms of Plerixafor octahydrochloride:

    Plerixafor octahydrochloride purchased from MCE. Usage Cited in: Brain Behav Immun. 2017 Jan;59:322-332.

    Pretreatment with TAK-242 restores the reduction of hippocampal MBP induced by ds-HMGB1. (A and B) MBP content is detected by Western blot analysis using antibodies against MBP. GAPDH is used to control the load quantity.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References


    Plerixafor octahydrochloride is a selective CXCR4 antagonist with IC50 of 44 nM.

    IC50 & Target

    IC50: 44 nM (CXCR4)[1]

    In Vitro

    The CXCR4 inhibitor Plerixafor (AMD3100) is a potent inhibitor of CXCL12-mediated chemotaxis (IC50, 5.7 nM) with a potency slightly better than its affinity for CXCR4. Treating the cells with CCX771 or CXCL11 has no effect on CXCL12-mediated MOLT-4 or U937 TEM. In contrast, 10 μM Plerixafor inhibits CXCL12-mediated TEM in both cells lines[1]. Plerixafor (10 μM)-treated cells show a moderate reduction in cell proliferation compared to CXCL12-stimulated cells, which do not reach statistical significance[2].

    In Vivo

    Plerixafor (2 mg/kg) administration to UUO mice exacerbates renal interstitial T cell infiltration, resulting in increased production of the pro-inflammatory cytokines IL-6 and IFN-γ and decreased expression of the anti-inflammatory cytokine IL-10[3]. Both perivascular and interstitial fibrosis are significantly reduced by the CXCR4 antagonist, Plerixafor (AMD3100) at 8 weeks[4]. LD50, mouse, SC: 16.3 mg/kg; LD50, rat, SC: >50 mg/kg; LD50, mouse and rat, IV injection: 5.2 mg/kg.

    Clinical Trial
    Cell Assay

    Plerixafor is dissolved in DMSO and then diluted with appropriate medium[2].

    U87MG 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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration

    Plerixafor is prepared in PBS (Mice)[3].
    Plerixafor (AMD3100) is prepared in H2O (Rats)[4].

    Male C57bl/6 mice (6-7 weeks old, weighing 20 g) are used. The animals are acclimated to the housing environment, which is SPF and had a temperature of 22°C and a 12h/12h light/dark cycle for a week. Then, they are randomly divided into following experimental groups, with 8 mice in each group: normal (no specific intervention), UUO+AMD3100 (mice received UUO surgery and 2 mg/kg AMD3100), and UUO+PBS (mice received UUO surgery and the same volume of PBS). AMD3100 and PBS are administered via intraperitoneal injection every day until sacrifice.
    The CXCR4 antagonist, AMD3100 dissolved in H2O, is delivered in the type 2 diabetic sand rat model at a dose of 6 mg/kg per day for 8 weeks. In complementary studies, the effect of CXCR4 antagonism (AMD3100 6mg/kg/d) on regulatory T cell numbers is examined. For these studies, AMD3100 or vehicle is delivered via minipump for a period of one week. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Molecular Weight




    CAS No.




    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    H2O: ≥ 42 mg/mL

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    Purity: 98.90%

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