Art. -Nr.: HY-10198

Navarixin

(Synonyms: SCH 527123; MK-7123)

32 Cited Publications

Kundenbewertung

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 K_d 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.

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Reinheit: 99.33%
CAS. Nr.: 473727-83-2
Formel: C₂₁H₂₃N₃O₅
Molecular Weight:397.42

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Navarixin Chemical Structure

CAS. Nr.: 473727-83-2

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (32)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]^[2]^[3]

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)

Alle CXCR Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	2.6 nM Compound: 4, SCH-527123	Displacement of [125I]hCXCL8 from human CXCR2 receptor expressed in BaF3 cells Displacement of [125I]hCXCL8 from human CXCR2 receptor expressed in BaF3 cells	[PMID: 17181143]
BaF3	IC₅₀	36 nM Compound: 4, SCH-527123	Displacement of [125I]hCXCL8 from human CXCR1 receptor expressed in BaF3 cells Displacement of [125I]hCXCL8 from human CXCR1 receptor expressed in BaF3 cells	[PMID: 17181143]
Caco-2	IC₅₀	18.78 μM Compound: Navarixin	Cytotoxicity against human Caco2 cells Cytotoxicity against human Caco2 cells	[PMID: 34536673]

In Vitro

Navarixin is a potent, allosteric antagonist of both CXCR1 and CXCR2, with K_d 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.

In Vivo

Navarixin (0.1-10 mg/kg, p.o.) blocks pulmonary neutrophilia (ED₅₀=1.2 mg/kg) and goblet cell hyperplasia (32-38% inhibition at 1-3 mg/kg) in mice following the intranasal lipopolysaccharide (LPS) administration. In rats, Navarixin (0.1-3 mg/kg p.o.) suppresses the pulmonary neutrophilia (ED=1.8 mg/kg) and increase in bronchoalveolar lavage (BAL) mucin content (ED₅₀=0.1 mg/kg) induced by intratracheal (i.t.) LPS^[1].

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 473727-83-2
Appearance Solid
Molecular Weight 397.42
Formel C₂₁H₂₃N₃O₅
Color White to yellow
SMILES

O=C1C(C(NC2=CC=CC(C(N(C)C)=O)=C2O)=C1N[C@H](CC)C3=CC=C(O3)C)=O
Synonyms

SCH 527123; MK-7123
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (32)

All Cell Proliferation/Viability AssayCell Migration/Invasion AssayBio/Physico-chemical AssayFlow CytometryHistological Imaging/Staining

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Journal Impact Factor

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.
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).
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
Adv Sci (Weinh)

Repurposing of Chemokine Antagonists for Combined Phase-Resolved Spinal Cord Injury Treatment. [Abstract]

2025 Oct 28:e16569. PMID: 41147460
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
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
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
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
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
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 Aug 12:178:117269. PMID: 39137654
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

Knockdown of EIF4G1 in NSCLC induces CXCL8 secretion. [Abstract]

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
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
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 Hard Tissue Biol

2020, 29(1):9-16.
bioRxiv

2026 Apr 7.
University of Regensburg

2025 Dec 3.
Patent

US20250154240A1.
bioRxiv

2025 March 11.
Patent

US20200281878A1.
Patent

US20180235964A1.
Patent

US20180221312A1.
Patent

US20170181987A1.
University of Calgary

Dec.23. 2015.

Lösungsmittel & Löslichkeit

In Vitro:

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.5162 mL

12.5811 mL

25.1623 mL

5 mM

0.5032 mL

2.5162 mL

5.0325 mL

10 mM

0.2516 mL

1.2581 mL

2.5162 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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 (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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.29 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Protocol 4

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline

Solubility: ≥ 2.5 mg/mL (6.29 mM); Clear solution

Protocol 5

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (6.29 mM); Clear solution

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Protokoll

Cell Assay^[2]

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.

Animal Administration^[1]

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.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (284 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

Navarixin

32 Cited Publications

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Navarixin

GPCR/G Protein Compound Library

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Publications Citing Use of MedChemExpress (MCE) Navarixin

Alle CXCR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (32)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Navarixin

GPCR/G Protein Compound Library

Immunology/Inflammation Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Small Molecule Immuno-Oncology Compound Library

Drug Repurposing Compound Library

Endocrinology Compound Library

Anti-COVID-19 Compound Library

Orally Active Compound Library

Anti-Prostate Cancer Compound Library

Chemokine Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Cytokine Inhibitors Library

Multi-Target Compound Library

Radioprotector Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) Navarixin

Alle CXCR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (32)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Navarixin Related Classifications

HY-10198 Related Classifications