2. GPCR/G Protein Immunology/Inflammation
  3. CCR
  4. BX471

BX471 (ZK-811752) is an orally active, potent and selective non-peptide CCR1 antagonist with a Ki of 1 nM, and exhibits 250-fold selectivity for CCR1 over CCR2, CCR5 and CXCR4.

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

CAS No. : 217645-70-0

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Customer Review

Based on 25 publication(s) in Google Scholar

Other Forms of BX471:

BX471 Related Antibodies

Top Publications Citing Use of Products

    BX471 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2025 Dec 22;16(1):918.  [Abstract]

    BX471 (50 mg/kg, i.p.) treatment significantly reduced tumor volume in WT mice, whereas recombinant CCL7 supplementation markedly increased tumors in Zbp1−/− mice.

    BX471 purchased from MedChemExpress. Usage Cited in: Mol Med. 2024 Jun 3;30(1):74.  [Abstract]

    Western blot was employed to determine the expression of P16INK4a and P21CIP1 treated with BX471 (5, 10 μM).

    BX471 purchased from MedChemExpress. Usage Cited in: Sci Adv. 2021 May 26;7(22):eabb5943.  [Abstract]

    Representative crystal violet staining and quantification of migrated B16-F10 cells in the Oris cell migration assay. B16-F10 cells were cultured in control medium or eosinophil culture supernatant after migration for 36 hours treated with or without 20 μM BX471.

    BX471 purchased from MedChemExpress. Usage Cited in: Cell Res. 2018 Mar;28(3):323-335.  [Abstract]

    Percentage of large, intermediate and small colonies in the single-colony forming assay of sorted LT-HSCs co-cultured with Eos and intervened with the CCL-6 antibody and BX471 (200 μM).

    BX471 purchased from MedChemExpress. Usage Cited in: Cell Res. 2018 Mar;28(3):323-335.  [Abstract]

    ROS MFI analysis in HSCs co-cultured for 2 h with Eos following treatment with BX471 (200 μM).

    View All CCR Isoform Specific Products:

    View All Isoforms
    CCR1 CCR2 CCR3 CCR4 CCR5 CCR6 CCR7 CCR8 CCR9

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    BX471 (ZK-811752) is an orally active, potent and selective non-peptide CCR1 antagonist with a Ki of 1 nM, and exhibits 250-fold selectivity for CCR1 over CCR2, CCR5 and CXCR4.

    IC50 & Target[1]

    MIP-1α-CCR1

    1 nM (Ki)

    RANTES-CCR1

    2.8 nM (Ki)

    MCP-3-CCR1

    5.5 nM (Ki)

    Cellular Effect
    Cell Line Type Value Description References
    HEK293 IC50
    5.5 nM
    Compound: 2, BX-471
    Displacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cells
    Displacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cells
    		[PMID: 19183043]
    THP-1 IC50
    1.5 nM
    Compound: 2, BX-471
    Antagonist activity at human CCR1 in THP1 cells assessed as inhibition of MIP-1-alpha-induced chemotaxis after 3 hrs
    Antagonist activity at human CCR1 in THP1 cells assessed as inhibition of MIP-1-alpha-induced chemotaxis after 3 hrs
    		[PMID: 19183043]
    THP-1 IC50
    18 nM
    Compound: BX-741
    Antagonist activity against human CCR1 receptor expressed in THP1 cells assessed as inhibition of chemotaxis
    Antagonist activity against human CCR1 receptor expressed in THP1 cells assessed as inhibition of chemotaxis
    		[PMID: 17446072]
    THP-1 IC50
    18 nM
    Compound: BX-741
    Antagonist activity at human CCR1 expressed in THP1 cells assessed as effect on MIP-1-alpha-induced calcium flux by FLIPR
    Antagonist activity at human CCR1 expressed in THP1 cells assessed as effect on MIP-1-alpha-induced calcium flux by FLIPR
    		[PMID: 17446072]
    In Vitro

    BX471 is a potent functional antagonist based on its ability to inhibit a number of CCR1-mediated effects including Ca2+ mobilization, increase in extracellular acidification rate, CD11b expression, and leukocyte migration. BX471 demonstrats a greater than 10,000-fold selectivity for CCR1 compared with 28 G-protein-coupled receptors[1].
    BX471 is also able to displace 125I-MIP-1α/CCL3 binding to mouse CCR1 in a concentration-dependent manner with a Ki of 215±46 nM. Increasing concentrations of BX471 inhibits the Ca2+ transients induced by MIP-1α/CCL3 in both human and mouse CCR1 with IC50 of 5.8±1 nM and 198±7 nM, respectively[2].
    BX471 (0.1-10 μM) shows a dose-dependent inhibition of RANTES-mediated and shear-resistant adhesion on IL-1β-activated microvascular endothelium in shear flow in isolated blood monocytes. BX471 also inhibits the RANTES-mediated adhesion of T lymphocytes to activated endothelium[4].

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

    BX471 Related Antibodies
    In Vivo

    BX471 (4 mg/kg, p.o. or i.v.) is orally active with a bioavailability of 60% in dogs. Furthermore, BX471 effectively reduces disease in a rat experimental allergic encephalomyelitis model of multiple sclerosis[1].
    BX471 (20 mg/kg, s.c.) reaches peak plasma levels of 9 μM by around 30 minutes, and this rapidly declines to approximately 0.4 μM after 2 hours. From 4 to 8 hours the drug plasma levels drops to 0.1 μM or lower. Mice treated with 20 mg/kg of BX471 for 10 days shows a reduction of interstitial CD45 positive leukocytes of approximately 55%. BX471 has a borderline significant effect on the number of CCR5-positive CD8 cells in the peripheral blood. BX471 reduces the amount of FSP1-positive cells by 65% in UUO kidneys as compared with vehicle control[2]. Pretreatment witih BX471 reduces macrophage and neutrophil accumulation in kidney after ischemia-reperfusion injury[3].

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

    434.89

    Formula

    C21H24ClFN4O3
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(N)NC1=CC(Cl)=CC=C1OCC(N2[C@H](C)CN(CC3=CC=C(F)C=C3)CC2)=O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 100 mg/mL (229.94 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : < 0.1 mg/mL (insoluble)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.2994 mL 11.4972 mL 22.9943 mL
    5 mM 0.4599 mL 2.2994 mL 4.5989 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

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

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

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    C2

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    Volume (final)

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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% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (5.75 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.08 mg/mL (4.78 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    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:  50% PEG300    50% Saline

      Solubility: 5 mg/mL (11.50 mM); Clear solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    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: 99.98%

    SDS (396 KB)

    COA (246 KB) HNMR (301 KB) RP-HPLC (255 KB) LCMS (95 KB)

    Handling Instructions (2659 KB)
    References
    Animal Administration
    [1]

    Fasted male beagle dogs (n=3 per treatment group) are given BX471 either by oral gavage or by intravenous injection via the cephalic vein at a dose of 4 mg/kg. The compound is dissolved in a vehicle of 40% aqueous cyclodextrin. Serial blood samples are collected utilizing an in-dwelling catheter in the jugular vein at the indicated time points up to 6 h post-dosing. EDTA is used as an anticoagulant. The samples are centrifuged (1000× g for 10 min at 4°C), and plasma is stored frozen until analyzed for drug levels by HPLC-MS (electrospray mode operated under a positive ion mode). Plasma samples are thawed and denatured by the addition of four parts of ice-cold methanol containing a fixed amount of an internal standard to one part of plasma. The resulting protein precipitate is removed by centrifugation at 5000× g, and the supernatants are analyzed directly. Concurrently plasma calibration standards of BX471 are prepared over the range of quantification, processed, and analyzed under identical conditions. A FISONS, VG Platform single quadrupole instrument is used in these analyses with an electrospray inlet operated at 3.57 kV. Chromatographic separation is accomplished using a YMC AQ octadecyl silane reversed phase column (4.6×250 mm) following a short isocratic elution method (35% methanol, 65% water containing 0.1% trifluoroacetic acid). The total column flow (1 mL/min) is split post-column to infuse 50 μL/min into the mass spectrometer. The chromatograms are collected over a total run time of 7.5 min/sample following a 50-μL injection on the column. The ions are collected in a single ion positive ionization mode. A calibration curve for quantification is generated by plotting ion current ratios between the internal standard peak and the analyte in the plasma standards over the quantification range. Calculations of percent oral availability is deduced from the area under curve measurements. Pharmacokinetic parameters are calculated using WinNonLin version 3.0.

    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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.2994 mL 11.4972 mL 22.9943 mL 57.4858 mL
    5 mM 0.4599 mL 2.2994 mL 4.5989 mL 11.4972 mL
    10 mM 0.2299 mL 1.1497 mL 2.2994 mL 5.7486 mL
    15 mM 0.1533 mL 0.7665 mL 1.5330 mL 3.8324 mL
    20 mM 0.1150 mL 0.5749 mL 1.1497 mL 2.8743 mL
    25 mM 0.0920 mL 0.4599 mL 0.9198 mL 2.2994 mL
    30 mM 0.0766 mL 0.3832 mL 0.7665 mL 1.9162 mL
    40 mM 0.0575 mL 0.2874 mL 0.5749 mL 1.4371 mL
    50 mM 0.0460 mL 0.2299 mL 0.4599 mL 1.1497 mL
    60 mM 0.0383 mL 0.1916 mL 0.3832 mL 0.9581 mL
    80 mM 0.0287 mL 0.1437 mL 0.2874 mL 0.7186 mL
    100 mM 0.0230 mL 0.1150 mL 0.2299 mL 0.5749 mL
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    BX471 Related Classifications

    Help & FAQs
    • 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.

    Keywords:

    BX471217645-70-0ZK-811752BX 471BX-471ZK811752ZK 811752CCRCC chemokine receptorInhibitorinhibitorinhibit

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