Navarixin
Based on 32 publication(s) in Google Scholar
Navarixin (SCH 527123) is a potent, allosteric and orally active antagonist of both CXCR1 and CXCR2, with Kd values of 41 nM for cynomolgus CXCR1 and 0.20 nM, 0.20 nM, 0.08 nM for mouse, rat and cynomolgus monkey CXCR2, respectivelly.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.33%
- CAS No.: 473727-83-2
- Formule: C21H23N3O5
- Masse moléculaire:397.42
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Publications Citing Use of MedChemExpress (MCE) Navarixin
More- Cancer Cell. 2024 Dec 9;42(12):2015-2031.e11. [Abstract]
- J Hepatol. 2023 Oct;79(4):1025-1036. [Abstract]
- Nat Immunol. 2019 Nov;20(11):1444-1455. [Abstract]
- Nat Microbiol. 2017 May 15:2:17072. [Abstract]
- Nat Commun. 2021 May 5;12(1):2547. [Abstract]
- Int J Oral Sci. 2026 Mar 1;18(1):22. [Abstract]
- Redox Biol. 2024 Aug:74:103209. [Abstract]
- Adv Sci (Weinh). 2025 Oct 28:e16569. [Abstract]
- Cell Death Dis. 2022 Jan 13;13(1):57. [Abstract]
- Cancer Lett. 2026 Mar 31:641:218269. [Abstract]
- J Allergy Clin Immunol. 2016 Jul;138(1):114-122.e4. [Abstract]
- Cell Commun Signal. 2024 Jan 17;22(1):43. [Abstract]
- Cell Rep. 2024 Dec 17;44(1):115072. [Abstract]
- J Invest Dermatol. 2025 Sep 30:S0022-202X(25)02476-5. [Abstract]
- Int J Mol Sci. 2023 Nov 27;24(23):16803. [Abstract]
- Front Pharmacol. 2024 Feb 9:15:1346383. [Abstract]
- Sci Rep. 2019 Dec 20;9(1):19500. [Abstract]
- ACS Pharmacol Transl Sci. 2024 Apr 18;7(5):1533-1545. [Abstract]
- Mol Pain. 2017 Jan-Dec:13:1744806917730212. [Abstract]
- PLoS One. 2021 Sep 29;16(9):e0237659. [Abstract]
- J Chromatogr B Analyt Technol Biomed Life Sci. 2015 Oct 1:1002:42-53. [Abstract]
- J Hard Tissue Biol. 2020, 29(1):9-16.
- bioRxiv. 2026 Apr 7.
- University of Regensburg. 2025 Dec 3.
- Patent. US20250154240A1.
- bioRxiv. 2025 March 11.
- Biomed Pharmacother. 2024 Sep:178:117269. [Abstract]
- Patent. US20200281878A1.
- Patent. US20180235964A1.
- Patent. US20180221312A1.
- Patent. US20170181987A1.
- University of Calgary. Dec.23. 2015.
Customer Validation & Images
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Cell Proliferation/Viability Assay
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Cell Migration/Invasion Assay
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Flow Cytometry
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Histological Imaging/Staining
Activité biologique
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125I-CXCL8-CXCR2 0.97 nM (IC50) |
Cynomolgus CXCR2 0.08 nM (Kd) |
Mouse CXCR2 0.2 nM (Kd) |
Rat CXCR2 0.2 nM (Kd) |
125I-CXCL8-CXCR1 43 nM (IC50) |
Cynomolgus CXCR1 41 nM (Kd) |
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Cell Line
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Type | Value | Description | References |
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| BaF3 | IC50 |
2.6 nM
Compound: 4, SCH-527123
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Displacement of [125I]hCXCL8 from human CXCR2 receptor expressed in BaF3 cells
Displacement of [125I]hCXCL8 from human CXCR2 receptor expressed in BaF3 cells
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[PMID: 17181143] |
| BaF3 | IC50 |
36 nM
Compound: 4, SCH-527123
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Displacement of [125I]hCXCL8 from human CXCR1 receptor expressed in BaF3 cells
Displacement of [125I]hCXCL8 from human CXCR1 receptor expressed in BaF3 cells
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[PMID: 17181143] |
| Caco-2 | IC50 |
18.78 μM
Compound: Navarixin
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Cytotoxicity against human Caco2 cells
Cytotoxicity against human Caco2 cells
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[PMID: 34536673] |
Navarixin is a potent, allosteric antagonist of both CXCR1 and CXCR2, with Kd values of 41 nM for cynomolgus CXCR1 and 0.20 nM, 0.20 nM, 0.08 nM for mouse, rat and cynomolgus monkey CXCR2, respectivelly[1]. Navarixin (1 nM) reduces CXCL8 potency in stimulating Ba/F3-hCXCR2 chemotaxis. Navarixin (3 nM) significantly inhibits the potency and efficacy of CXCL1-induced neutrophils (PMN) chemotaxis. Navarixin (300 nM) significantly decreases chemokine potency and slightly decreases maximal cell movement for Ba/F3-CXCR1 cells[2]. Navarixin (25 μM) is sufficient to block IL-8-mediated CXCR2 activation in HCT116, E2, Caco2, and IIIe cells, in which phosphorylation of downstream kinases of CXCR2 is reduced in a concentration-dependent manner[3].
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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 473727-83-2
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Appearance Solid
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Masse moléculaire 397.42
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Formule C21H23N3O5
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Color White to yellow
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SMILES
O=C1C(C(NC2=CC=CC(C(N(C)C)=O)=C2O)=C1N[C@H](CC)C3=CC=C(O3)C)=O
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Synonyms
SCH 527123; MK-7123
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (32)
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Journal Impact Factor
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Most Recent
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Cancer Cell
Interleukin-1α release during necrotic-like cell death generates myeloid-driven immunosuppression that restricts anti-tumor immunity. [Abstract]2024 Dec 9;42(12):2015-2031.e11. PMID: 39577420
Navarixin purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2024 Dec 9;42(12):2015-2031.e11. [Abstract]
Navarixin (1 mg/200 mL; i.g.; once daily) significantly restricted the growth of PyMT-B6-ZsGreen tumors undergoing RIPK3-induced necroptosis.
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J Hepatol
Ductular reaction-associated neutrophils promote biliary epithelium proliferation in chronic liver disease. [Abstract]2023 Oct;79(4):1025-1036. PMID: 37348790
Navarixin purchased from MedChemExpress. Usage Cited in: J Hepatol. 2023 Oct;79(4):1025-1036. [Abstract]
CXCR1/2 inhibitor Navarixin (SCH 527123) (50 μM; 2 h) abrogated neutrophil migration by organoid-conditioned medium.
Navarixin purchased from MedChemExpress. Usage Cited in: J Hepatol. 2023 Oct;79(4):1025-1036. [Abstract]
Navarixin (SCH 527123) (50 μM; 6 h) partially prevented increased expression of Il6, Tnfa, Il1b and Cxcl1 in neutrophils stimulated with organoid-conditioned medium.
Navarixin purchased from MedChemExpress. Usage Cited in: J Hepatol. 2023 Oct;79(4):1025-1036. [Abstract]
Navarixin (SCH 527123) (50 μM; 18 h) partially prevented lower levels of L-selectin and increased expression of CD11b, CXCR4, and CCR2 in neutrophils stimulated with organoid-conditioned medium.
Navarixin purchased from MedChemExpress. Usage Cited in: J Hepatol. 2023 Oct;79(4):1025-1036. [Abstract]
Immunofluorescence of progenitor markers in liver sections of mice fed with DDC for 3 weeks and treated with Navarixin (SCH 527123) (50 mg/kg; i.g.; once daily for 3 weeks).
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Nat Immunol
Locally instructed CXCR4hi neutrophils trigger environment-driven allergic asthma through the release of neutrophil extracellular traps. [Abstract]2019 Nov;20(11):1444-1455. PMID: 31591573 -
Nat Microbiol
Nitric oxide prevents a pathogen-permissive granulocytic inflammation during tuberculosis. [Abstract]2017 May 15:2:17072. PMID: 28504669 -
Nat Commun
Selection of a picomolar antibody that targets CXCR2-mediated neutrophil activation and alleviates EAE symptoms. [Abstract]2021 May 5;12(1):2547. PMID: 33953162 -
Int J Oral Sci
Single-cell transcriptional atlas reveals distinct immune-chondrocyte crosstalk mechanisms in temporomandibular joint osteoarthritis induced by different types of occlusal disorder. [Abstract]2026 Mar 1;18(1):22. PMID: 41764220 -
Redox Biol
Lactate-induced activation of tumor-associated fibroblasts and IL-8-mediated macrophage recruitment promote lung cancer progression. [Abstract]2024 Aug:74:103209. PMID: 38861833 -
Adv Sci (Weinh)
Repurposing of Chemokine Antagonists for Combined Phase-Resolved Spinal Cord Injury Treatment. [Abstract]2025 Oct 28:e16569. PMID: 41147460 -
Cell Death Dis
Cancer-derived exosomal HSPC111 promotes colorectal cancer liver metastasis by reprogramming lipid metabolism in cancer-associated fibroblasts. [Abstract]2022 Jan 13;13(1):57. PMID: 35027547 -
Cancer Lett
NR4A2 induces perineural invasion in head and neck squamous cell carcinoma and pancreatic ductal adenocarcinoma via CXCL5/CXCR2 signaling axis. [Abstract]2026 Mar 31:641:218269. PMID: 41580014 -
J Allergy Clin Immunol
Chemokine release from human rhinovirus-infected airway epithelial cells promotes fibroblast migration. [Abstract]2016 Jul;138(1):114-122.e4. PMID: 26883463 -
Cell Commun Signal
Systematic assessment of chemokine ligand bias at the human chemokine receptor CXCR2 indicates G protein bias over β-arrestin recruitment and receptor internalization. [Abstract]2024 Jan 17;22(1):43. PMID: 38233929 -
Cell Rep
Pathogenic role for CD101-negative neutrophils in the type I interferon-mediated immunopathogenesis of tuberculosis. [Abstract]2024 Dec 17;44(1):115072. PMID: 39693225 -
J Invest Dermatol
PGE2/EP3/CXCR2 axis dictates amplified inflammatory response during skin infection in obese mice. [Abstract]2025 Sep 30:S0022-202X(25)02476-5. PMID: 41038339 -
Int J Mol Sci
CXCR2-Blocking Has Context-Sensitive Effects on Rat Glioblastoma Cell Line Outgrowth (S635) in an Organotypic Rat Brain Slice Culture Depending on Microglia-Depletion (PLX5622) and Dexamethasone Treatment. [Abstract]2023 Nov 27;24(23):16803. PMID: 38069130 -
Front Pharmacol
2024 Feb 9:15:1346383. PMID: 38405671 -
Sci Rep
Mild Traumatic Brain Injury Causes Nociceptive Sensitization through Spinal Chemokine Upregulation. [Abstract]2019 Dec 20;9(1):19500. PMID: 31863005 -
ACS Pharmacol Transl Sci
Development of a Fluorescent Ligand for the Intracellular Allosteric Binding Site of the Neurotensin Receptor 1. [Abstract]2024 Apr 18;7(5):1533-1545. PMID: 38751637 -
Mol Pain
The Chemokine Receptor CXCR2 Supports Nociceptive Sensitization after Traumatic Brain Injury. [Abstract]2017 Jan-Dec:13:1744806917730212. PMID: 28845733 -
PLoS One
Anti-inflammatory activity of lefamulin versus azithromycin and dexamethasone in vivo and in vitro in a lipopolysaccharide-induced lung neutrophilia mouse model. [Abstract]2021 Sep 29;16(9):e0237659. PMID: 34587166 -
J Chromatogr B Analyt Technol Biomed Life Sci
At-line coupling of LC-MS to bioaffinity and selectivity assessment for metabolic profiling of ligands towards chemokine receptors CXCR1 and CXCR2. [Abstract]2015 Oct 1:1002:42-53. PMID: 26301479 -
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Biomed Pharmacother
1-palmitoyl-2-linoleoyl-3-acetyl-rac-glycerol treatment inhibits abnormal tumor growth by regulating neutrophil infiltration in a non-small cell lung carcinoma mouse model. [Abstract]2024 Sep:178:117269. PMID: 39137654 -
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Solvant et solubilité
DMSO : ≥ 50 mg/mL (125.81 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.29 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (6.29 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Please enter the basic information of animal experiments:
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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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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocole
Recombinant cells are resuspended at 1×106/mL in assay buffer (phenol red free-RPMI 1640 supplemented with 2% FBS). Human neutrophils are resuspended at 2 × 106/mL in the same assay buffer containing 5% FBS. CXCL1 binds only CXCR2 with high affinity, whereas CXCL8 binds both CXCR1 and CXCR2 with high affinity. Chemoattractants (30 μL) diluted in assay buffer are dispensed into the bottom wells of disposable microchemotaxis plates, which are then covered with filter. Cells are preincubated with Navarixin (1-300 nM) in a CO2 incubator for 90 min. Cell aliquots (25 μL) are applied to each spot on the filter. After incubation (90 min for BaF/3 cells and 30 min for PMN in a CO2 incubator), the filters are removed[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[1]
Male BALB/c mice weighing between 20 and 25 g are used. Control mice receive intranasal injection of 50 μL of isotonic (0.9%) saline. Navarixin (0.1-10 mg/kg, p.o.) is suspended in 0.4% methylcellulose and given orally by gavage 2 h before and 4 h after each intranasal administration of LPS. Control animals receive 0.4% methylcellulose (10 mL/kg). In total, four doses of Navarixin or vehicle are given[1].
Rats[1]
Male Sprague-Dawley rats (200 g) are used. Control animals receive 100 μL of isotonic saline. Navarixin (0.1-3 mg/kg, p.o.) is suspended in 0.4% methylcellulose vehicle and given orally 2 h before the LPS challenge. Control rats receive oral methylcellulose (10 mL/kg). Only one dose of Navarixin or vehicle is given in these experiments[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (284 KB)
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SDS (640 KB)
- English - EN (640 KB)
- Français - FR (640 KB)
- Deutsch - DE (640 KB)
- Norwegian - NO (640 KB)
- Español - ES (640 KB)
- Swedish - SV (640 KB)
- Italian - IT (640 KB)
- Korean - KR (640 KB)
- Portuguese - PT (640 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Gonsiorek W, et al. Pharmacological characterization of Sch527123, a potent allosteric CXCR1/CXCR2 antagonist. J Pharmacol Exp Ther. 2007 Aug;322(2):477-85. [Content Brief]
[2]. Chapman RW, et al. A novel, orally active CXCR1/2 receptor antagonist, Sch527123, inhibits neutrophil recruitment, mucus production, and goblet cell hyperplasia in animal models of pulmonary inflammation. J Pharmacol Exp Ther. 2007 Aug;322(2):486-93. [Content Brief]
[3]. Ning Y, et al. The CXCR2 antagonist, SCH-527123, shows antitumor activity and sensitizes cells to NSC 266046 in preclinical colon cancer models. Mol Cancer Ther. 2012 Jun;11(6):1353-64. [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, 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 | 2.5162 mL | 12.5811 mL | 25.1623 mL | 62.9057 mL |
| 5 mM | 0.5032 mL | 2.5162 mL | 5.0325 mL | 12.5811 mL | |
| 10 mM | 0.2516 mL | 1.2581 mL | 2.5162 mL | 6.2906 mL | |
| 15 mM | 0.1677 mL | 0.8387 mL | 1.6775 mL | 4.1937 mL | |
| 20 mM | 0.1258 mL | 0.6291 mL | 1.2581 mL | 3.1453 mL | |
| 25 mM | 0.1006 mL | 0.5032 mL | 1.0065 mL | 2.5162 mL | |
| 30 mM | 0.0839 mL | 0.4194 mL | 0.8387 mL | 2.0969 mL | |
| 40 mM | 0.0629 mL | 0.3145 mL | 0.6291 mL | 1.5726 mL | |
| 50 mM | 0.0503 mL | 0.2516 mL | 0.5032 mL | 1.2581 mL | |
| 60 mM | 0.0419 mL | 0.2097 mL | 0.4194 mL | 1.0484 mL | |
| 80 mM | 0.0315 mL | 0.1573 mL | 0.3145 mL | 0.7863 mL | |
| 100 mM | 0.0252 mL | 0.1258 mL | 0.2516 mL | 0.6291 mL |
Navarixin Related Classifications
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