Home Immunology & Inflammation CXCR inhibitor Reparixin (Repertaxin) For research use only.

Reparixin (Repertaxin)

Synonyms: DF 1681Y

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).

Reparixin (Repertaxin) Chemical Structure

Reparixin (Repertaxin) Chemical Structure

CAS No. 266359-83-5

Purity & Quality Control

Reparixin (Repertaxin) Related Products

Signaling Pathway

CXCR Signaling Pathways

CXCR Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
polymorphonuclear cells Function assay Inhibition of CXCL8-induced chemotaxis in human polymorphonuclear cells, IC50=0.0053μM 15974585
L1.2 Function assay Inhibition of CXCL8-induced cell migration in L1.2 cells expressing CXCR1 by chemotaxis assay, IC50=0.0056μM 17665889
L1.2 Function assay Inhibition of CXCL8-induced cell migration in L1.2 cells expressing Ile43Val CXCR1 mutant by chemotaxis assay, IC50=0.08μM 17665889
L1.2 Function assay up to 1000 nM Inhibition of CXCL8-induced cell migration in L1.2 cells expressing wild type CXCR1 at up to 1000 nM by chemotaxis assay 17665889
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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
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].
Cell Research 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.
Experimental Result Images Methods Biomarkers Images PMID
Western blot IL-8 / STAT3 / p-STAT3 / AKT / p-AKT CXCR1 / CACR2 / Bcl-2 / Bax / Cyclin D1 / VEGF / MMP-2 / MMP-9 / TIMP-2 / E-cadherin / p-ERK / ERK 30397072
Immunofluorescence p-FAK / p-AKT / FOXO3A 20051626
In Vivo
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)
Animal Research Animal Models SHR rats
Dosages 5 mg/kg
Administration s.c.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05835466 Recruiting
Myelofibrosis (PMF)|Post Essential Thrombocythemia Myelofibrosis (ET-MF)|Post Polycythemia Vera Related Myelofibrosis (PV-MF)
Icahn School of Medicine at Mount Sinai|Dompé Farmaceutici S.p.A
 June 27 2023 Phase 2
NCT05496868 Recruiting
Acute Respiratory Distress Syndrome Adult
Dompé Farmaceutici S.p.A
 February 7 2023 Phase 2
NCT01861054 Terminated
Breast Cancer
Dompé Farmaceutici S.p.A
 February 2013 Phase 2

Chemical Information & Solubility

Molecular Weight 283.39 Formula

C14H21NO3S
CAS No. 266359-83-5 SDF Download Reparixin (Repertaxin) SDF
Smiles CC(C)CC1=CC=C(C=C1)C(C)C(=O)NS(=O)(=O)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (352.87 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 57 mg/mL

Water : Insoluble


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In vivo
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Tech Support

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.

Handling Instructions

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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).

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