BX471 hydrochloride
Based on 26 publication(s) in Google Scholar
BX471 hydrochloride (ZK-811752 hydrochloride) is a potent, selective non-peptide CCR1 antagonist with Ki of 1 nM for human CCR1, and exhibits 250-fold selectivity for CCR1 over CCR2, CCR5 and CXCR4.
For research use only. We do not sell to patients.
- Purity: 99.94%
- CAS No.: 288262-96-4
- Formula: C21H25Cl2FN4O3
- Molecular Weight:471.35
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Storage:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Publications Citing Use of MedChemExpress (MCE) BX471 hydrochloride
More- Signal Transduct Target Ther. 2021 Feb 28;6(1):91. [Abstract]
- Cancer Cell. 2021 Mar 8;39(3):423-437.e7. [Abstract]
- Immunity. 2026 Mar 10;59(3):598-617.e11. [Abstract]
- Cell Res. 2018 Mar;28(3):323-335. [Abstract]
- Neuron. 2025 Nov 18:S0896-6273(25)00803-7. [Abstract]
- J Exp Clin Cancer Res. 2022 Mar 3;41(1):81. [Abstract]
- Sci Adv. 2021 May 26;7(22):eabb5943. [Abstract]
- J Biomed Sci. 2026 Jan 9;33(1):10. [Abstract]
- Cancer Lett. 2025 Sep 25:634:218064. [Abstract]
- Cell Death Dis. 2025 Dec 22;16(1):918. [Abstract]
- Proc Natl Acad Sci U S A. 2025 Aug 26;122(34):e2503779122. [Abstract]
- Mol Med. 2024 Dec 20;30(1):253. [Abstract]
- Mol Med. 2024 Jun 3;30(1):74. [Abstract]
- J Agric Food Chem. 2024 Apr 15. [Abstract]
- J Invest Dermatol. 2025 Nov 28:S0022-202X(25)03613-9. [Abstract]
- Commun Biol. 2026 May 15;9(1):661. [Abstract]
- Int J Mol Sci. 2024 Apr 14;25(8):4337. [Abstract]
- Int Immunopharmacol. 2026 May 1:176:116478. [Abstract]
- Int Immunopharmacol. 2025 Jan 12:147:114027. [Abstract]
- Neuropharmacology. 2024 Nov 26:264:110239. [Abstract]
- Lab Invest. 2020 Apr;100(4):619-629. [Abstract]
- J Inflamm Res. 2020 Jul 21;13:343-356. [Abstract]
- Sci Rep. 2020 Nov 25;10(1):20508. [Abstract]
- Immunol Lett. 2018 Dec:204:29-37. [Abstract]
- bioRxiv. 2024 November 03.
- Research Square Preprint. 2021 Oct.
Customer Validation & Images
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In Vivo Efficacy Study
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WB
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Cell Migration/Invasion Assay
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Cell Proliferation/Viability Assay
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Cell Imaging/Staining
Biological Activity
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MIP-1α-CCR1 1 nM (Ki) |
RANTES-CCR1 2.8 nM (Ki) |
MCP-3-CCR1 5.5 nM (Ki) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO-K1 | IC50 |
0.04 μM
Compound: BX-471
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Antagonistic activity at human CCR1 in CHO-K1 cells
Antagonistic activity at human CCR1 in CHO-K1 cells
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[PMID: 16198561] |
| CHO-K1 | IC50 |
0.55 μM
Compound: BX-471
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Antagonistic activity at rat CCR1 in CHO-K1 cells
Antagonistic activity at rat CCR1 in CHO-K1 cells
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[PMID: 16198561] |
| CHO-K1 | IC50 |
1.5 μM
Compound: BX-471
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Antagonistic activity at mouse CCR1 in CHO-K1 cells
Antagonistic activity at mouse CCR1 in CHO-K1 cells
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[PMID: 16198561] |
| THP-1 | IC50 |
0.0004 μM
Compound: BX-471
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Antagonistic activity at human CCR1 by inhibition of MIP-1alpha induced calcium mobilization in THP1 cells
Antagonistic activity at human CCR1 by inhibition of MIP-1alpha induced calcium mobilization in THP1 cells
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[PMID: 16198561] |
| THP-1 | IC50 |
0.4 nM
Compound: BX-471
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Antagonistic activity at human CCR1 by inhibition of MIP-1alpha induced calcium mobilization in THP1 cells
Antagonistic activity at human CCR1 by inhibition of MIP-1alpha induced calcium mobilization in THP1 cells
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[PMID: 16198561] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 288262-96-4
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Appearance Solid
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Molecular Weight 471.35
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Formula C21H25Cl2FN4O3
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Color White to yellow
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SMILES
O=C(N)NC1=CC(Cl)=CC=C1OCC(N2[C@H](C)CN(CC3=CC=C(F)C=C3)CC2)=O.Cl
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Synonyms
ZK-811752 hydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (26)
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Journal Impact Factor
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Most Recent
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Signal Transduct Target Ther
Eosinophil-derived chemokine (hCCL15/23, mCCL6) interacts with CCR1 to promote eosinophilic airway inflammation. [Abstract]2021 Feb 28;6(1):91. PMID: 33640900 -
Cancer Cell
Cathepsin C promotes breast cancer lung metastasis by modulating neutrophil infiltration and neutrophil extracellular trap formation. [Abstract]2021 Mar 8;39(3):423-437.e7. PMID: 33450198 -
Immunity
2026 Mar 10;59(3):598-617.e11. PMID: 41722568 -
Cell Res
2018 Mar;28(3):323-335. PMID: 29327730
BX471 hydrochloride 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 hydrochloride 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).
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Neuron
2025 Nov 18:S0896-6273(25)00803-7. PMID: 41260217 -
J Exp Clin Cancer Res
Tumor bud-derived CCL5 recruits fibroblasts and promotes colorectal cancer progression via CCR5-SLC25A24 signaling. [Abstract]2022 Mar 3;41(1):81. PMID: 35241150 -
Sci Adv
2021 May 26;7(22):eabb5943. PMID: 34039594
BX471 hydrochloride 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.
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J Biomed Sci
2026 Jan 9;33(1):10. PMID: 41508046 -
Cancer Lett
Tumor-derived CCL5 recruits CCR1+ macrophages to suppress apoptosis and drive proliferation in duodenal adenocarcinoma. [Abstract]2025 Sep 25:634:218064. PMID: 41015267 -
Cell Death Dis
2025 Dec 22;16(1):918. PMID: 41430036
BX471 hydrochloride 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.
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Proc Natl Acad Sci U S A
Unraveling the neuroimmune mechanisms in cancer-induced bone pain: New horizons for therapeutic intervention of the two-phase paradigm. [Abstract]2025 Aug 26;122(34):e2503779122. PMID: 40828016 -
Mol Med
CXCL4 deficiency limits M4 macrophage infiltration and attenuates hyperoxia-induced lung injury. [Abstract]2024 Dec 20;30(1):253. PMID: 39707183 -
Mol Med
Inhibition of CC chemokine receptor 1 ameliorates osteoarthritis in mouse by activating PPAR-γ. [Abstract]2024 Jun 3;30(1):74. PMID: 38831316
BX471 hydrochloride 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).
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J Agric Food Chem
Palmatine Attenuated Lipopolysaccharide-Induced Acute Lung Injury by Inhibiting M1 Phenotype Macrophage Polarization via NAMPT/TLR2/CCR1 Signaling. [Abstract]2024 Apr 15. PMID: 38619332 -
J Invest Dermatol
Multiomics reveals CCL3-driving neuronal sensitization in chronic pruritus of unknown origin. [Abstract]2025 Nov 28:S0022-202X(25)03613-9. PMID: 41320115 -
Commun Biol
2026 May 15;9(1):661. PMID: 42141167 -
Int J Mol Sci
Novel Findings on CCR1 Receptor in CNS Disorders: A Pathogenic Marker Useful in Controlling Neuroimmune and Neuroinflammatory Mechanisms in Parkinson's Disease. [Abstract]2024 Apr 14;25(8):4337. PMID: 38673922 -
Int Immunopharmacol
2026 May 1:176:116478. PMID: 41825208 -
Int Immunopharmacol
Blocking the CCL5/CCL7-CCR1 axis regulates macrophage polarization through NF-κB pathway to alleviate the progression of osteoarthritis. [Abstract]2025 Jan 12:147:114027. PMID: 39805173 -
Neuropharmacology
CCR1 antagonist as a potential modulator of inflammatory, autophagic, and apoptotic markers in spinal cord injury. [Abstract]2024 Nov 26:264:110239. PMID: 39608704 -
Lab Invest
CCL8 secreted by tumor-associated macrophages promotes invasion and stemness of glioblastoma cells via ERK1/2 signaling. [Abstract]2020 Apr;100(4):619-629. PMID: 31748682 -
J Inflamm Res
Therapeutic Effect of C-C Chemokine Receptor Type 1 (CCR1) Antagonist BX471 on Allergic Rhinitis. [Abstract]2020 Jul 21;13:343-356. PMID: 32801828 -
Sci Rep
Multiple myeloma hinders erythropoiesis and causes anaemia owing to high levels of CCL3 in the bone marrow microenvironment. [Abstract]2020 Nov 25;10(1):20508. PMID: 33239656 -
Immunol Lett
2018 Dec:204:29-37. PMID: 30321562 -
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Solvent & Solubility
DMSO : 116.67 mg/mL (247.52 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocol
Briefly, dermal microvascular endothelial cells grown to confluence in Petri dishes are stimulated with IL-1β (10 ng/mL) for 12 h followed by pre-incubation with RANTES (10 nM) for 30 min at 37°C just prior to assay. The plates are assembled as the lower wall in a parallel wall flow chamber and mounted on the stage of an Olympus IMT-2 inverted microscope with ×20 and ×40 phase-contrast objectives. Isolated human blood monocytes are isolated and resuspended at 5×105 cells/mL in assay buffer (HBSS) containing 10 mM HEPES, pH 7.4 and 0.5% human serum albumin. Shortly before the assay, 1 mM Mg2+ and 1 mM Ca2+ are added. The cell suspensions are kept in a heating block at 37°C during the assay and perfused into the flow chamber at a rate of 1.5 dyn/cm2 for 5 min. For inhibition experiments, monocytes are preincubated with BX471 at different concentrations (0.1-10 μM) or a Me2SO control for 10 min at 37°C. The number of firmLy adherent cells after 5 min is quantitated in multiple fields (at least five per experiment) by analysis of images recorded with a long integration JVC 3CCD video camera and a JVC SR L 900 E video recorder and are expressed as cells/mm2. The type of adhesion analyzed is restricted to primary, i.e. direct interactions of monocytes with endothelium.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (281 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Liang M, et al. Identification and characterization of a potent, selective, and orally active antagonist of the CC chemokine receptor-1. J Biol Chem. 2000 Jun 23;275(25):19000-8. [Content Brief]
[2]. Anders HJ, et al. A chemokine receptor CCR-1 antagonist reduces renal fibrosis after unilateral ureter ligation. J Clin Invest. 2002 Jan;109(2):251-9. [Content Brief]
[3]. Furuichi K, et al. Chemokine receptor CCR1 regulates inflammatory cell infiltration after renal ischemia-reperfusion injury. J Immunol. 2008 Dec 15;181(12):8670-6. [Content Brief]
[4]. Horuk R, et al. A non-peptide functional antagonist of the CCR1 chemokine receptor is effective in rat heart transplant rejection. J Biol Chem. 2001 Feb 9;276(6):4199-204. [Content Brief]
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 (sealed storage, away from moisture). 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 | 1 mM | 2.1216 mL | 10.6078 mL | 21.2157 mL | 53.0391 mL |
| 5 mM | 0.4243 mL | 2.1216 mL | 4.2431 mL | 10.6078 mL | |
| 10 mM | 0.2122 mL | 1.0608 mL | 2.1216 mL | 5.3039 mL | |
| 15 mM | 0.1414 mL | 0.7072 mL | 1.4144 mL | 3.5359 mL | |
| 20 mM | 0.1061 mL | 0.5304 mL | 1.0608 mL | 2.6520 mL | |
| 25 mM | 0.0849 mL | 0.4243 mL | 0.8486 mL | 2.1216 mL | |
| 30 mM | 0.0707 mL | 0.3536 mL | 0.7072 mL | 1.7680 mL | |
| 40 mM | 0.0530 mL | 0.2652 mL | 0.5304 mL | 1.3260 mL | |
| 50 mM | 0.0424 mL | 0.2122 mL | 0.4243 mL | 1.0608 mL | |
| 60 mM | 0.0354 mL | 0.1768 mL | 0.3536 mL | 0.8840 mL | |
| 80 mM | 0.0265 mL | 0.1326 mL | 0.2652 mL | 0.6630 mL | |
| 100 mM | 0.0212 mL | 0.1061 mL | 0.2122 mL | 0.5304 mL |
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