Reparixin (Repertaxin)

Catalog No.S8640

Reparixin (Repertaxin) Chemical Structure

Molecular Weight(MW): 283.39

Reparixin(Repertaxin) is a inhibitor of human CXCR1/R2 and rat CXCR2 receptor activation. It also inhibits human CXCL8 receptor activation.

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Biological Activity

Description Reparixin(Repertaxin) is a inhibitor of human CXCR1/R2 and rat CXCR2 receptor activation. It also inhibits human CXCL8 receptor activation.
Targets
CXCR1 [1]
()
CXCR2 [1]
()
CXCL8 [1]
()
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

Cell Research:

[1]

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  • 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.


    (Only for Reference)
Animal Research:

[1]

+ Expand
  • Animal Models: SHR rats
  • Formulation: saline
  • Dosages: 5 mg/kg
  • Administration: s.c.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 56 mg/mL (197.6 mM)
Ethanol 56 mg/mL (197.6 mM)
Water 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.

Chemical Information

Molecular Weight 283.39
Formula

C14H21NO3S

CAS No. 266359-83-5
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02370238 Active not recruiting Metastatic Breast Cancer Dompé Farmaceutici S.p.A|PRA Health Sciences June 2015 Phase 2
NCT03031470 Completed Ischemia-reperfusion Injury in Liver Transplant|Early Allograft Dysfunction Dompé Farmaceutici S.p.A March 2015 Phase 2
NCT01967888 Completed Pancreatectomy for Chronic Pancreatitis Dompé Farmaceutici S.p.A February 2014 Phase 2|Phase 3
NCT01861054 Terminated Breast Cancer Dompé Farmaceutici S.p.A February 2013 Phase 2
NCT01817959 Completed Islet Transplantation in Diabetes Mellitus Type 1 Dompé Farmaceutici S.p.A October 2012 Phase 3
NCT02001974 Completed Metastatic Breast Cancer Dompé Farmaceutici S.p.A|PRA Health Sciences January 2012 Phase 1

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Frequently Asked Questions

  • Question 1:

    Do you have the information of the half life time of reparixin Catalog No.S8640 in rats?

  • Answer:

    The following paper indicated the half-life of this compound in rats is 0.5h (http://jpet.aspetjournals.org/content/322/3/973).

CXCR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID