Reparixin (Repertaxin)

Catalog No.S8640 Batch:S864002

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Technical Data

Formula

C14H21NO3S
Molecular Weight 283.39 CAS No. 266359-83-5
Solubility (25°C)* In vitro DMSO 100 mg/mL (352.87 mM)
Ethanol 57 mg/mL (201.13 mM)
Water Insoluble
* <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.)

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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 is a non-competitive allosteric blocker of CXCR1 and CXCR2 receptor activation, which inhibits intracellular signal pathways without affecting receptor bindings. Reparixin potently and selectively inhibits a wide range of biological activities that are induced by CXCL8 such as leukocytes recruitment and functional inflammatory reactions. However, reparixin does not affect CXCR1/CXCR2 activation induced by other chemotactic factors, C5a, fMLP, CXCL12 or several other agonists of GPCRs. Reparixin can regulate the production of angiotensin II receptors, which may influence Ang II-induced hypertension[1]. Reparixin specifically blocks CXCR1/2-mediated mouse and human neutrophil migration in vitro without affecting other receptors. Reparixin inhibits CXCL8-induced neutrophil activation through human CXCR1 and human CXCR2 and blocks phosphorylation of downstream signalling molecules. Reparixin prevents the increase of intracellular free calcium, elastase release and production of reactive oxygen intermediates, but leaves phagocytosis of Escherichia coli bacteria unaffected[2].
In vivo

Reparixin, an inhibitor of CXCL8 receptor CXCR1 and CXCR2 activation, attenuates inflammatory responses in various injury models. Reparixin 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)[1]. (SHR: Spontaneously hypertensive rats)

Protocol (from reference)

Cell Assay:

[1]
  • Cell lines

    HUVECs

  • Concentrations

    1 μM

  • Incubation Time

    30 min

  • Method

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

[1]
  • Animal Models

    SHR rats

  • Dosages

    5 mg/kg

  • Administration

    s.c.

Selleck's Reparixin (Repertaxin) has been cited by 13 publications

Bronchial epithelial transcriptomics and experimental validation reveal asthma severity-related neutrophilc signatures and potential treatments [ Commun Biol, 2024, 7(1):181] PubMed: 38351296
Metabolic lactate production coordinates vasculature development and progenitor behavior in the developing mouse neocortex [ Nat Neurosci, 2022, 25(7):865-875] PubMed: 35726058
On the origin of metastases: Induction of pro-metastatic states after impending cell death via ER stress, reprogramming, and a cytokine storm [ Cell Rep, 2022, 38(10):110490] PubMed: 35263600
Biphasic Effect of Pirfenidone on Angiogenesis [ Cell Death Discov, 2022, 8(1):235] PubMed: 35487914
Erastin enhances metastatic potential of ferroptosis-resistant ovarian cancer cells by M2 polarization through STAT3/IL-8 axis [ Int Immunopharmacol, 2022, 113(Pt B):109422] PubMed: 36410184
Overexpression of BQ323636.1 Modulated AR/IL-8/CXCR1 Axis to Confer Tamoxifen Resistance in ER-Positive Breast Cancer [ Life (Basel), 2022, 12(1)93] PubMed: 35054486
Cancer-associated fibroblasts promote the survival of irradiated nasopharyngeal carcinoma cells via the NF-κB pathway [ J Exp Clin Cancer Res, 2021, 40(1):87] PubMed: 33648530
Self-sustaining IL-8 loops drive a prothrombotic neutrophil phenotype in severe COVID-19 [ JCI Insight, 2021, 6(18)e150862] PubMed: 34403366
HER2 overexpression triggers the IL-8 to promote arsenic-induced EMT and stem cell-like phenotypes in human bladder epithelial cells [ Ecotoxicol Environ Saf, 2021, 208:111693] PubMed: 33396024
Probiotics improve re-epithelialization of scratches infected by Porphyromonas gingivalis through up-regulating CXCL8-CXCR1/CXCR2 axis [ Anaerobe, 2021, 72:102458] PubMed: 34547426

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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.