Reparixin (Repertaxin)

Catalog No.S8640 Batch:S864001

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Technical Data

Formula

C14H21NO3S
Molecular Weight 283.39 CAS No. 266359-83-5
Solubility (25°C)* In vitro DMSO 56 mg/mL (197.6 mM)
Ethanol 56 mg/mL (197.6 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Reparixin (Repertaxin, DF 1681Y) is a potent and specific inhibitor of CXCR1 with IC50 of 1 nM. Reparixin (Repertaxin) inhibits PMN migration induced by CXCL8 (IC50 = 1 nM) and rodent PMN chemotaxis induced by CXCL1 and CXCL2. Repertaxin inhibits the response of human PMN to CXCL1, which interacts with CXCR2 (IC50 = 400 nM).
Targets
CXCR1 [3]
(Cell-free assay)		 CXCL8 [3]
(Cell-free assay)		 CXCR2 [3]
(Cell-free assay)
1 nM 1 nM 400 nM
In vitro

Reparixin (Repertaxin) is a non-competitive allosteric blocker of CXCR1 and CXCR2 receptor activation, which inhibits intracellular signal pathways without affecting receptor bindings. It potently and selectively inhibits a wide range of biological activities that are induced by CXCL8 such as leukocytes recruitment and functional inflammatory reactions. However, this compound does not affect CXCR1/CXCR2 activation induced by other chemotactic factors, C5a, fMLP, CXCL12 or several other agonists of GPCRs. It can regulate the production of angiotensin II receptors, which may influence Ang II-induced hypertension. Reparixin specifically blocks CXCR1/2-mediated mouse and human neutrophil migration in vitro without affecting other receptors. The compound inhibits CXCL8-induced neutrophil activation through human CXCR1 and human CXCR2 and blocks phosphorylation of downstream signalling molecules. It prevents the increase of intracellular free calcium, elastase release and production of reactive oxygen intermediates, but leaves phagocytosis of Escherichia coli bacteria unaffected.
In vivo

Reparixin (Repertaxin), an inhibitor of CXCL8 receptor CXCR1 and CXCR2 activation, attenuates inflammatory responses in various injury models. It effectively decreases systolic blood pressure and increases the blood flow. The thoracic aorta wall thickness is significantly decreased in SHR-R (the reparixin-treated group) compared to SHR-N (normal saline-treated SHR). (SHR: Spontaneously hypertensive rats)

Protocol (from reference)

Cell Assay:

[1]
  • Cell lines

    HUVECs

  • Concentrations

    1 μM

  • Incubation Time

    30 min

  • Method

    After pretreatment of HUVECs without or with reparixin (1 μM) for 30 min, cells were treated with or without Ang II (100 nmol/l) or CXCL8 (100 ng/ml) for 2 h. Total RNA was then isolated, and real-time PCR was performed.
Animal Study:

[1]
  • Animal Models

    SHR rats

  • Dosages

    5 mg/kg

  • Administration

    s.c.

References

  • https://pubmed.ncbi.nlm.nih.gov/21212529/
  • https://pubmed.ncbi.nlm.nih.gov/18587419/
  • https://pubmed.ncbi.nlm.nih.gov/15282370/

Selleck's Reparixin (Repertaxin) Has Been Cited by 29 Publications

Tryptophan 2,3-dioxygenase 2 controls M2 macrophages polarization to promote esophageal squamous cell carcinoma progression via AKT/GSK3β/IL-8 signaling pathway [ Acta Pharmaceutica Sinica B, September 2021, 2835-2849] PubMed: 34589400
NMI induces chemokine release and recruits neutrophils through the activation of NF-κB pathway [ bioRxiv, September 18, 2024, nan]
TRIM26 alleviates fatal immunopathology by regulating inflammatory neutrophil infiltration during Candida infection [ PLoS Pathogens, January 2, 2024, e1011902] PubMed: 38166150
HER2 overexpression triggers the IL-8 to promote arsenic-induced EMT and stem cell-like phenotypes in human bladder epithelial cells [ Ecotoxicology and Environmental Safety, January 15, 2021, 111693] PubMed: 33396024
Bronchial epithelial transcriptomics and experimental validation reveal asthma severity-related neutrophilc signatures and potential treatments [ Communications Biology, February 2024, 181] PubMed: 38351296
Immunothrombolytic monocyte-neutrophil axes dominate the single-cell landscape of human thrombosis and correlate with thrombus resolution [ Immunity, 2025, S1074-7613(25)00139-6] PubMed: 40280129
Harnessing the FGFR2/NF2/YAP signaling-dependent necroptosis to develop an FGFR2/IL-8 dual blockade therapeutic strategy [ Nat Commun, 2025, 16(1):4128] PubMed: 40319089
Nucleus-translocated glucokinase functions as a protein kinase to phosphorylate TAZ and promote tumour growth [ Nat Commun, 2025, 16(1):7156] PubMed: 40759645
Induction of cell death by the CXCR2 antagonist SB225002 in colorectal cancer and stromal cells [ Biomed Pharmacother, 2025, 188:118203] PubMed: 40412356
Chromosomal instability shapes the tumor microenvironment of esophageal adenocarcinoma via a cGAS-chemokine-myeloid axis [ bioRxiv, 2025, 2025.05.06.652454] PubMed: 40654626

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.