1. GPCR/G Protein
    Immunology/Inflammation
  2. CXCR

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

Cat. No.: HY-50912 Purity: 98.90%
Data Sheet SDS 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

    Description

    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
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    References
    Cell Assay
    [2]

    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
    [3][4]

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

    Mice[3]
    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.
    Rat[4]
    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.

    References
    Molecular Weight

    794.47

    Formula

    C₂₈H₆₂Cl₈N₈

    CAS No.

    155148-31-5

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

    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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    Inquiry Information

    Product Name:
    Plerixafor octahydrochloride
    Cat. No.:
    HY-50912
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