1. GPCR/G Protein
    Immunology/Inflammation
    Anti-infection
  2. CXCR
    HIV
    Virus Protease
  3. Plerixafor

Plerixafor (Synonyms: AMD 3100; JM3100; SID791)

Cat. No.: HY-10046 Purity: >98.0%
Handling Instructions

Plerixafor (AMD 3100) est un antagoniste sélectif de CXCR4 avec un IC50 de 44 nM. Plerixafor, un immunostimulant et un mobilisateur de cellules souches hématopoïétiques (CSH), est un agoniste allostérique du CXCR7. Plerixafor inhibe la réplication de VIH-1 et de VIH-2 avec une EC50 de 1-10 nM.

Plerixafor (AMD 3100) ist ein selektiver CXCR4-Antagonist mit einer IC50 von 44 nM. Plerixafor, ein Immunstimulans und ein Mobilisator für hematopoietic stem cell (HSC), ist ein allosterischer Agonist von CXCR7. Plerixafor hemmt die HIV-1- und HIV-2-Replikation mit einem EC50-Wert von 1-10 nM.

Plerixafor (AMD 3100) is a selective CXCR4 antagonist with an IC50 of 44 nM. Plerixafor, an immunostimulant and a hematopoietic stem cell (HSC) mobilizer, is an allosteric agonist of CXCR7. Plerixafor inhibits HIV-1 and HIV-2 replication with an EC50 of 1-10 nM.

For research use only. We do not sell to patients.

Plerixafor Chemical Structure

Plerixafor Chemical Structure

CAS No. : 110078-46-1

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Customer Review

Based on 24 publication(s) in Google Scholar

Other Forms of Plerixafor:

Top Publications Citing Use of Products

    Plerixafor 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 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.

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    Description

    Plerixafor (AMD 3100) is a selective CXCR4 antagonist with an IC50 of 44 nM. Plerixafor, an immunostimulant and a hematopoietic stem cell (HSC) mobilizer, is an allosteric agonist of CXCR7. Plerixafor inhibits HIV-1 and HIV-2 replication with an EC50 of 1-10 nM[1][2][3][4][7].

    IC50 & Target

    125I-CXCL12-CXCR4

    44 nM (IC50)

    125I-CXCL12-CXCR7

     

    HIV-1

    1-10 nM (EC50)

    HIV-2

    1-10 nM (EC50)

    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. Plerixafor interferes with the interaction of CXCR4 with its natural ligand, SDF-1 (CXCL12). 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].

    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[5].
    Both perivascular and interstitial fibrosis are significantly reduced by the CXCR4 antagonist, Plerixafor (AMD3100) at 8 weeks[6]. 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
    Molecular Weight

    502.78

    Formula

    C₂₈H₅₄N₈

    CAS No.

    110078-46-1

    SMILES

    C1(CN2CCCNCCNCCCNCC2)=CC=C(C=C1)CN3CCNCCCNCCNCCC3

    Shipping

    Room temperature in continental US; may vary elsewhere.

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

    Ethanol : ≥ 166.66 mg/mL (331.48 mM)

    DMSO : < 1 mg/mL (insoluble or slightly soluble)

    H2O : < 0.1 mg/mL (insoluble)

    DMF : < 1 mg/mL (insoluble)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.9889 mL 9.9447 mL 19.8894 mL
    5 mM 0.3978 mL 1.9889 mL 3.9779 mL
    10 mM 0.1989 mL 0.9945 mL 1.9889 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Plerixafor (AMD3100) is dissolved in DMSO and in sterile PBS for animal administration[6].

    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. 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

    Purity: >98.0%

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    Keywords:

    PlerixaforAMD 3100JM3100SID791AMD3100AMD-3100JM 3100JM-3100SID 791SID-791CXCRHIVVirus ProteaseCXC chemokine receptorsC-X-C motif chemokine receptorsHuman immunodeficiency virushumancancerstemcellsligandmobilizerperipheralbloodstreamG-CSFlymphomamultiplemyelomaInhibitorinhibitorinhibit

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