Reparixin (Repertaxin)

Catalog No.S8640 Synonyms: DF 1681Y

For research use only.

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

CAS No. 266359-83-5

Selleck's Reparixin (Repertaxin) has been cited by 10 Publications

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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].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
polymorphonuclear cells MYTGeY5kfGmxbjDhd5NigQ>? MkXDTY5pcWKrdHnvckBw\iCFWFPMPE1qdmS3Y3XkJINp\W2xdHH4bZMhcW5iaIXtZY4heG:ueX3vdpBpd263Y3zlZZIh[2WubIOsJGlEPTB;MD6wNFU{|ryP M13Vc|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF3OUe0OVg2Lz5zNUm3OFU5PTxxYU6=
L1.2 MULGeY5kfGmxbjDhd5NigQ>? M1zl[GlvcGmkaYTpc44hd2ZiQ2jDUFgucW6mdXPl[EBk\WyuIH3p[5JifGmxbjDpckBNOS5{IHPlcIx{KGW6cILld5NqdmdiQ2jDVlEh[nliY3jlcY91[XirczDhd5NigSxiSVO1NF0xNjByNUdOwG0> M3XIfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5Nk[1PFg6Lz5zN{[2OVg5QTxxYU6=
L1.2 M1[2b2Z2dmO2aX;uJIF{e2G7 MmnYTY5pcWKrdHnvckBw\iCFWFPMPE1qdmS3Y3XkJINmdGxibXnndoF1cW:wIHnuJGwyNjJiY3XscJMh\XiycnXzd4lv\yCLbHW0N3ZidCCFWFPSNUBufXSjboSgZpkh[2inbX;0ZZhqeyCjc4PhfUwhUUN3ME2wMlA5|ryP NFrONIU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{[2OVg5QSd-MUe2OlU5QDl:L3G+
L1.2 M2\kNGZ2dmO2aX;uJIF{e2G7 NIXIboh2eCC2bzCxNFAxKG6P MlS2TY5pcWKrdHnvckBw\iCFWFPMPE1qdmS3Y3XkJINmdGxibXnndoF1cW:wIHnuJGwyNjJiY3XscJMh\XiycnXzd4lv\yC5aXzkJJR6eGViQ2jDVlEh[XRidYCgeI8hOTByMDDuUUBjgSClaHXtc5RigGm|IHHzd4F6 MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzZ4NUi4PUc,OTd4NkW4PFk9N2F-
Assay
Methods Test Index 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 26847910
Immunofluorescence p-FAK / p-AKT / FOXO3A 20051626
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 Research:

[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 Research:

[1]

  • Animal Models: SHR rats
  • Dosages: 5 mg/kg
  • Administration: s.c.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 283.39
Formula

C14H21NO3S

CAS No. 266359-83-5
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(C)CC1=CC=C(C=C1)C(C)C(=O)NS(=O)(=O)C

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01861054 Terminated Drug: Reparixin Breast Cancer Dompé Farmaceutici S.p.A February 2013 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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.

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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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