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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|Description||Reparixin(Repertaxin) is a inhibitor of human CXCR1/R2 and rat CXCR2 receptor activation. It also inhibits human CXCL8 receptor activation.|
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. 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.
|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). (SHR: Spontaneously hypertensive rats)|
|In vitro||DMSO||56 mg/mL (197.6 mM)|
|Ethanol||56 mg/mL (197.6 mM)|
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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|
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
Do you have the information of the half life time of reparixin Catalog No.S8640 in rats?
The following paper indicated the half-life of this compound in rats is 0.5h (http://jpet.aspetjournals.org/content/322/3/973).