1. GPCR/G Protein
    Immunology/Inflammation
  2. CXCR
  3. Plerixafor octahydrochloride

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

Cat. No.: HY-50912 Purity: >98.0%
Handling Instructions

Plerixafor octahydrochloride (AMD3100 octahydrochloride) is a selective CXCR4 antagonist with an 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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10 mM * 1 mL in Water USD 84 In-stock
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Estimated Time of Arrival: December 31
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Customer Review

Based on 15 publication(s) in Google Scholar

Other Forms of Plerixafor octahydrochloride:

Top Publications Citing Use of Products

    Plerixafor octahydrochloride purchased from MCE. Usage Cited in: Int J Biol Sci. 2017 May 5;13(5):604-614.

    Epithelial cells with or without AMD3100 pretreatment are cultured in conditioned medium (CM) from LPS-treated NFs or LTA-treated NFs for 3 days, and the secretion of TNF-α in the supernatant of culture is detected by ELISA. Epithelial cells cultured in MSM are used as control. Both LPS-treated NFs and LTA-treated NFs enhanced the section of TNF-α by epithelial cells compared with control. Pretreatment of epithelial cells with AMD3100 significantly attenuates the increase of TNF-α.

    Plerixafor octahydrochloride purchased from MCE. Usage Cited in: Cell Physiol Biochem. 2018;46(3):890-906.

    The protein expression of LRRC4, SDF-1, CXCR4, ERK, Slit2 and VEGF in the brain tissue of rats is determined by Western blotting.

    View All CXCR Isoform Specific Products:

    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    Plerixafor octahydrochloride (AMD3100 octahydrochloride) is a selective CXCR4 antagonist with an IC50 of 44 nM.

    IC50 & Target[1]

    125I-CXCL12-CXCR4

    44 nM (IC50)

    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
    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    H2O : ≥ 42 mg/mL (52.87 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.2587 mL 6.2935 mL 12.5870 mL
    5 mM 0.2517 mL 1.2587 mL 2.5174 mL
    10 mM 0.1259 mL 0.6294 mL 1.2587 mL
    *Please refer to the solubility information to select the appropriate solvent.
    References
    Cell Assay
    [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]

    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.
    Rats[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

    SMILES

    [H]Cl.[H]Cl.[H]Cl.[H]Cl.[H]Cl.[H]Cl.[H]Cl.[H]Cl.N1(CCCNCCNCCCNCC1)CC2=CC=C(C=C2)CN3CCCNCCNCCCNCC3

    Shipping

    Room temperature in continental US; may vary elsewhere

    Purity: >98.0%

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

    Cat. No.: HY-50912