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

Plerixafor  (Synonyms: AMD 3100; JM3100; SID791)

Cat. No.: HY-10046 Purity: 99.90%
SDS COA 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

Size Price Stock Quantity
5 mg USD 54 In-stock
10 mg USD 79 In-stock
25 mg USD 142 In-stock
50 mg USD 199 In-stock
100 mg USD 279 In-stock
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Customer Review

Based on 79 publication(s) in Google Scholar

Other Forms of Plerixafor:

Top Publications Citing Use of Products

67 Publications Citing Use of MCE Plerixafor

RT-PCR
WB
IF
Proliferation Assay
IHC

    Plerixafor purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2022 Oct 7;551:215944.  [Abstract]

    Immunohistochemical staining of proliferation-related protein, Ki-67, in breast cancer after treatment with control, AMD3100 (2.5 mg/kg), Olaparib, or a combination of AMD3100 and Olaparib.

    Plerixafor purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2022 Oct 7;551:215944.  [Abstract]

    Viability of cells treated with combinations different concentrations of AMD3100 and Olaparib for 24 h.

    Plerixafor purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2022 Feb 4;13(2):118.  [Abstract]

    PGK1 induced the CXCR4-mediated phosphorylation of AKT (p-AKT) and ERK (p-ERK), and blockade of CXCR4 signaling by AMD3100 (48 h) treatment did not alter cellular PGK1 expression in KIRC cells.

    Plerixafor purchased from MedChemExpress. Usage Cited in: Bioact Mater. 2021 Jan 7;6(7):2039-2057.  [Abstract]

    Western blot analysis of the expression of CXCR4, integrin αvβ3, p-Jak2, Jak2, p-FAK, FAK, p-STAT3 and STAT3 in MSCs (pretreated with a CXCR4 inhibitor (AMD3100; 20 μM; pretreated with 1 h) and an integrin αvβ3 inhibitor (cyclo(-RGDfK))) after the addition of 152RM for 24 h.

    Plerixafor purchased from MedChemExpress. Usage Cited in: Theranostics. 2021 Jan 1;11(6):2612-2633.  [Abstract]

    Caco-2 cells are incubated with vehicle or AMD3100 (1 µg/ml, 24 hours) after lentivirus transfection (LV-HOXB5), then Western blotting assays are conducted to measure the protein levels of CXCL12, HOXB5, CXCR4, p-ERK and p-ETS1 in the indicated cell lines.

    Plerixafor purchased from MedChemExpress. Usage Cited in: Theranostics. 2021 Jan 1;11(6):2612-2633.  [Abstract]

    Transwell assays indicated that AMD3100 treatment (1 µg/ml, 24 hours) significantly decreases the migration and invasion of Caco-2-HOXB5 cells.

    Plerixafor purchased from MedChemExpress. Usage Cited in: Adv Funct Mater. 2020, 2000309.

    NOD/SCID mice were i.p. injected with AMD3100 (4 mg/kg). After 1 h, the mice are i.v. injected with iFluor 647-labeled Aazo@CMSN. At 12 h after nanoparticle injection, the mouse craniums are excised for the observation of nanoparticle bone marrow niches targeting under CLSM. Pre-treatment with AMD3100 significantly declined the bone marrow niches targeting of the nanoparticles.

    Plerixafor purchased from MedChemExpress. Usage Cited in: Cell Mol Immunol. 2020 Mar;17(3):283-299.  [Abstract]

    ELISA of IL-1β in supernatants of BV2 cells stimulated with gp120 LAV (0.5 μg/mL) for 24 h in the presence of increasing doses of a CXCR4-specific inhibitor (AMD3100, 0.1-10 μM; prestimulated with 30 min-2 h).

    Plerixafor purchased from MedChemExpress. Usage Cited in: Oncogene. 2019 Jun;38(25):5021-5037.  [Abstract]

    IF staining of the tumor tissue sections showed decreased Ki67 and a reversal of EMT markers indicated by increased E-cadherin and decreased N-cadherin expression in the AMD3100 (5 mg/kg or 3.5 mg/kg) treated groups.

    Plerixafor purchased from MedChemExpress. Usage Cited in: Oncogene. 2019 Jun;38(25):5021-5037.  [Abstract]

    Additional EMT-related proteins (Snail and Slug) are downregulated by AMD3100 (5 mg/kg or 3.5 mg/kg) in tumor samples from both diet groups, as quantified by immunoblotting.

    Plerixafor purchased from MedChemExpress. Usage Cited in: Cell Physiol Biochem. 2018;46(3):890-906.  [Abstract]

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

    Plerixafor purchased from MedChemExpress. Usage Cited in: Int J Biol Sci. 2017 May 5;13(5):604-614.  [Abstract]

    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.

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    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    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[3][7]

    125I-CXCL12-CXCR4

    44 nM (IC50)

    125I-CXCL12-CXCR7

     

    HIV-1

    1-10 nM (EC50)

    HIV-2

    1-10 nM (EC50)

    Cellular Effect
    Cell Line Type Value Description References
    CEM-SS CC50
    > 5 μM
    Compound: AMD-3100
    Cytotoxicity against human CEM-SS cells by MTT assay
    Cytotoxicity against human CEM-SS cells by MTT assay
    [PMID: 19356827]
    CHO IC50
    0.051 μM
    Compound: AMD3100
    Competitive binding affinity to CXCR4 receptor (unknown origin) expressed in CHO cells incubated for 40 mins by 12G5 antibody based fluorescence analysis
    Competitive binding affinity to CXCR4 receptor (unknown origin) expressed in CHO cells incubated for 40 mins by 12G5 antibody based fluorescence analysis
    [PMID: 30978562]
    CHO IC50
    65 nM
    Compound: AMD3100
    Binding affinity to CXCR4 (unknown origin) expressed in CHO cells measured after 40 mins by 12G5 antibody competition assay
    Binding affinity to CXCR4 (unknown origin) expressed in CHO cells measured after 40 mins by 12G5 antibody competition assay
    [PMID: 27658790]
    HEK293 IC50
    2.3 nM
    Compound: AMD-3100
    Antiviral activity against T20-resistant HIV1 NL4-3 infected in HEK293 cells assessed as inhibition of viral replication after 2 days
    Antiviral activity against T20-resistant HIV1 NL4-3 infected in HEK293 cells assessed as inhibition of viral replication after 2 days
    [PMID: 19451305]
    HEK293 IC50
    213.1 nM
    Compound: 1; AMD3100
    Displacement of [125I]CXCL12 from human CXCR4 expressed in HEK293 cell membranes after 1.5 hrs by Topcount method
    Displacement of [125I]CXCL12 from human CXCR4 expressed in HEK293 cell membranes after 1.5 hrs by Topcount method
    [PMID: 29314840]
    HEK293 IC50
    4.6 nM
    Compound: AMD-3100
    Antiviral activity against HIV1 NL4-3 infected in HEK293 cells assessed as inhibition of viral replication after 2 days
    Antiviral activity against HIV1 NL4-3 infected in HEK293 cells assessed as inhibition of viral replication after 2 days
    [PMID: 19451305]
    HEK293 IC50
    5.3 nM
    Compound: AMD-3100
    Antiviral activity against multidrug resistant HIV1 HXB2 infected in HEK293 cells assessed as inhibition of viral replication after 2 days
    Antiviral activity against multidrug resistant HIV1 HXB2 infected in HEK293 cells assessed as inhibition of viral replication after 2 days
    [PMID: 19451305]
    HEK293 IC50
    6.2 nM
    Compound: AMD-3100
    Antiviral activity against HIV1 HXB2 infected in HEK293 cells assessed as inhibition of viral replication after 2 days
    Antiviral activity against HIV1 HXB2 infected in HEK293 cells assessed as inhibition of viral replication after 2 days
    [PMID: 19451305]
    HEK293 IC50
    7 nM
    Compound: AMD-3100
    Antiviral activity against NNRTI-resistant HIV1 HXB2 infected in HEK293 cells assessed as inhibition of viral replication after 2 days
    Antiviral activity against NNRTI-resistant HIV1 HXB2 infected in HEK293 cells assessed as inhibition of viral replication after 2 days
    [PMID: 19451305]
    HEK293 IC50
    9 nM
    Compound: AMD-3100
    Antiviral activity against NRTI-resistant HIV1 HXB2 infected in HEK293 cells assessed as inhibition of viral replication after 2 days
    Antiviral activity against NRTI-resistant HIV1 HXB2 infected in HEK293 cells assessed as inhibition of viral replication after 2 days
    [PMID: 19451305]
    HEK293 IC50
    9.2 nM
    Compound: AMD-3100
    Antiviral activity against PI-resistant HIV1 HXB2 infected in HEK293 cells assessed as inhibition of viral replication after 2 days
    Antiviral activity against PI-resistant HIV1 HXB2 infected in HEK293 cells assessed as inhibition of viral replication after 2 days
    [PMID: 19451305]
    MT4 CC50
    > 10 μg/mL
    Compound: AMD-3100
    Cytotoxicity against human MT4 cells by MTT assay
    Cytotoxicity against human MT4 cells by MTT assay
    [PMID: 23157587]
    MT4 CC50
    > 421 μM
    Compound: 1, AMD-3100
    Cytotoxicity against human MT4 cells after 4 days by MTT method
    Cytotoxicity against human MT4 cells after 4 days by MTT method
    [PMID: 20043638]
    MT4 CC50
    > 421 μM
    Compound: 10d
    Concentration required to reduce the viability of mock infected cells by 50%
    Concentration required to reduce the viability of mock infected cells by 50%
    [PMID: 8568797]
    MT4 CC50
    > 50 μM
    Compound: AMD3100
    Cytotoxicity against human MT4 cells by MTT assay in presence of 2.5 uM of chloroquine
    Cytotoxicity against human MT4 cells by MTT assay in presence of 2.5 uM of chloroquine
    [PMID: 26094944]
    MT4 CC50
    > 50 μM
    Compound: AMD3100
    Cytotoxicity against human MT4 cells by MTT assay in presence of 5 uM of chloroquine
    Cytotoxicity against human MT4 cells by MTT assay in presence of 5 uM of chloroquine
    [PMID: 26094944]
    MT4 CC50
    > 50 μM
    Compound: AMD3100
    Cytotoxicity against human MT4 cells by MTT assay in presence of 10 uM of chloroquine
    Cytotoxicity against human MT4 cells by MTT assay in presence of 10 uM of chloroquine
    [PMID: 26094944]
    MT4 CC50
    > 50 μM
    Compound: AMD3100
    Cytotoxicity against in human MT-4 after 5 days by MTT assay
    Cytotoxicity against in human MT-4 after 5 days by MTT assay
    [PMID: 33316719]
    MT4 CC50
    > 50 μM
    Compound: AMD3100
    Cytotoxicity against Human immunodeficiency virus 1 NL4-3 infected in human MT4 cells assessed as reduction in cell viability measured after 5 days by MTT assay
    Cytotoxicity against Human immunodeficiency virus 1 NL4-3 infected in human MT4 cells assessed as reduction in cell viability measured after 5 days by MTT assay
    [PMID: 32305183]
    MT4 CC50
    > 50 μM
    Compound: AMD3100
    Cytotoxicity against human MT4 cells by MTT assay
    Cytotoxicity against human MT4 cells by MTT assay
    [PMID: 26094944]
    MT4 EC50
    0.004 μM
    Compound: 1, AMD-3100
    Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus replication after 4 days by MTT assay
    Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus replication after 4 days by MTT assay
    [PMID: 20043638]
    MT4 EC50
    0.008 μM
    Compound: AMD3100
    Antiviral activity against HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay after 20 passages selected in presence of compound
    Antiviral activity against HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay after 20 passages selected in presence of compound
    [PMID: 18378713]
    MT4 EC50
    0.008 μM
    Compound: AMD3100
    Antiviral activity against HIV 1 RIN HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay after 40 passages selected in presence of compound
    Antiviral activity against HIV 1 RIN HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay after 40 passages selected in presence of compound
    [PMID: 18378713]
    MT4 EC50
    0.008 μM
    Compound: AMD3100
    Antiviral activity against HIV 1 RIN HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay after 60 passages selected in presence of compound
    Antiviral activity against HIV 1 RIN HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay after 60 passages selected in presence of compound
    [PMID: 18378713]
    MT4 EC50
    0.014 μM
    Compound: AMD3100
    Antiviral activity against HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay
    Antiviral activity against HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay
    [PMID: 18378713]
    MT4 IC50
    0.017 μg/mL
    Compound: AMD-3100
    Antiviral activity against X4 HIV1 NL4.3 infected in human MT4 cells assessed as inhibition of viral replication pre-incubated for 30 mins measured 5 days post infection by MTT assay
    Antiviral activity against X4 HIV1 NL4.3 infected in human MT4 cells assessed as inhibition of viral replication pre-incubated for 30 mins measured 5 days post infection by MTT assay
    [PMID: 23157587]
    MT4 EC50
    0.025 μM
    Compound: AMD3100
    Antiviral activity against T-cell line-tropic HIV1 NL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 5 days by MTT assay in presence of 5 uM of chloroquine
    Antiviral activity against T-cell line-tropic HIV1 NL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 5 days by MTT assay in presence of 5 uM of chloroquine
    [PMID: 26094944]
    MT4 EC50
    0.028 μM
    Compound: AMD3100
    Antiviral activity against HIV 1 3B harboring integrase L34M mutant infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay selected after 40 passages in presence of compound
    Antiviral activity against HIV 1 3B harboring integrase L34M mutant infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay selected after 40 passages in presence of compound
    [PMID: 18378713]
    MT4 EC50
    0.032 μM
    Compound: AMD3100
    Antiviral activity against T-cell line-tropic HIV1 NL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 5 days by MTT assay
    Antiviral activity against T-cell line-tropic HIV1 NL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 5 days by MTT assay
    [PMID: 26094944]
    MT4 EC50
    0.034 μM
    Compound: AMD3100
    Antiviral activity against HIV 1 3B infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay
    Antiviral activity against HIV 1 3B infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay
    [PMID: 18378713]
    MT4 EC50
    0.039 μM
    Compound: AMD3100
    Antiviral activity against T-cell line-tropic HIV1 NL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 5 days by MTT assay in presence of 2.5 uM of chloroquine
    Antiviral activity against T-cell line-tropic HIV1 NL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 5 days by MTT assay in presence of 2.5 uM of chloroquine
    [PMID: 26094944]
    MT4 EC50
    0.049 μM
    Compound: AMD3100
    Antiviral activity against HIV 1 3B harboring integrase E92Q S230N double mutant infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay selected after 20 passages in presence of compound
    Antiviral activity against HIV 1 3B harboring integrase E92Q S230N double mutant infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay selected after 20 passages in presence of compound
    [PMID: 18378713]
    MT4 EC50
    0.056 μM
    Compound: AMD3100
    Antiviral activity against HIV 1 3B harboring integrase E92Q, S230N and L34M triple mutant infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay selected after 60 passages in presence of compound
    Antiviral activity against HIV 1 3B harboring integrase E92Q, S230N and L34M triple mutant infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay selected after 60 passages in presence of compound
    [PMID: 18378713]
    MT4 EC50
    10 μM
    Compound: 37
    Concentration required to inhibit syncytia formation by 50% on HIV-1 infected MT-4 cells
    Concentration required to inhibit syncytia formation by 50% on HIV-1 infected MT-4 cells
    [PMID: 9925728]
    MT4 EC50
    2 nM
    Compound: AMD3100; 15c; 16c
    Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay
    Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay
    [PMID: 26974376]
    MT4 EC50
    2 nM
    Compound: AMD3100; 15c; 16c
    Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay
    Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay
    [PMID: 26974376]
    MT4 CC50
    6.5 μM
    Compound: AMD-3100
    Cytotoxicity against human MT4 cells by MTT assay
    Cytotoxicity against human MT4 cells by MTT assay
    [PMID: 19356827]
    PBMC CC50
    > 10 μg/mL
    Compound: AMD-3100
    Cytotoxicity against human PBMC cells by MTT assay
    Cytotoxicity against human PBMC cells by MTT assay
    [PMID: 23157587]
    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]
    . Plerixafor prevents the infiltration of tumor-associated macrophages (TAMs) into the tumor tissues[8].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    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.

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Clinical Trial
    Molecular Weight

    502.78

    Formula

    C28H54N8

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    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 : 50 mg/mL (99.45 mM; Need ultrasonic)

    DMSO : 1.92 mg/mL (3.82 mM; ultrasonic and warming and adjust pH to 7 with 1 M HCL and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : < 0.1 mg/mL (insoluble)

    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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% EtOH    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 3 mg/mL (5.97 mM); Clear solution

      This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (30.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% EtOH    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 3 mg/mL (5.97 mM); Clear solution

      This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (30.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
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    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.90%

    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

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO / Ethanol 1 mM 1.9889 mL 9.9447 mL 19.8894 mL 49.7235 mL
    Ethanol 5 mM 0.3978 mL 1.9889 mL 3.9779 mL 9.9447 mL
    10 mM 0.1989 mL 0.9945 mL 1.9889 mL 4.9724 mL
    15 mM 0.1326 mL 0.6630 mL 1.3260 mL 3.3149 mL
    20 mM 0.0994 mL 0.4972 mL 0.9945 mL 2.4862 mL
    25 mM 0.0796 mL 0.3978 mL 0.7956 mL 1.9889 mL
    30 mM 0.0663 mL 0.3315 mL 0.6630 mL 1.6575 mL
    40 mM 0.0497 mL 0.2486 mL 0.4972 mL 1.2431 mL
    50 mM 0.0398 mL 0.1989 mL 0.3978 mL 0.9945 mL
    60 mM 0.0331 mL 0.1657 mL 0.3315 mL 0.8287 mL
    80 mM 0.0249 mL 0.1243 mL 0.2486 mL 0.6215 mL
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    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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