Reparixin (Repertaxin)

Katalognr.S8640 Batch:S864001

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Tekniska data

Formel

C14H21NO3S
Molekylvikt 283.39 CAS-nr. 266359-83-5
Löslighet (25°C)* In vitro DMSO 56 mg/mL (197.6 mM)
Ethanol 56 mg/mL (197.6 mM)
Water Insoluble
In Vivo (Tillsätt lösningsmedel till produkten individuellt och i ordning.)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml betyder svårlösligt eller olösligt.
* Vänligen notera att Selleck testar lösligheten för alla förbindelser internt, och den faktiska lösligheten kan skilja sig något från publicerade värden. Detta är normalt och beror på små variationer mellan olika partier.
* Rumstempererad frakt (Stabilitetstester visar att denna produkt kan fraktas utan några kylåtgärder.)

Beredning av stamlösningar

Biologisk aktivitet

Beskrivning Reparixin (Repertaxin, DF 1681Y) är en potent och specifik hämmare av CXCR1 med ett IC50-värde på 1 nM. Reparixin (Repertaxin) hämmar PMN-migration inducerad av CXCL8 (IC50 = 1 nM) samt gnagar-PMN-kemotaxi inducerad av CXCL1 och CXCL2. Repertaxin hämmar responsen hos humana PMN vid exponering för CXCL1, vilket interagerar med CXCR2 (IC50 = 400 nM).
Mål
CXCR1
(Cell-free assay)		 CXCL8
(Cell-free assay)		 CXCR2
(Cell-free assay)
1 nM 1 nM 400 nM
In vitro

Reparixin (Repertaxin) is a non-competitive allosteric blocker of CXCR1 and CXCR2 receptor activation, which inhibits intracellular signal pathways without affecting receptor bindings. It potently and selectively inhibits a wide range of biological activities that are induced by CXCL8 such as leukocytes recruitment and functional inflammatory reactions. However, this compound does not affect CXCR1/CXCR2 activation induced by other chemotactic factors, C5a, fMLP, CXCL12 or several other agonists of GPCRs. It 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. The compound inhibits CXCL8-induced neutrophil activation through human CXCR1 and human CXCR2 and blocks phosphorylation of downstream signalling molecules. It 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 (Repertaxin), an inhibitor of CXCL8 receptor CXCR1 and CXCR2 activation, attenuates inflammatory responses in various injury models. It 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)

Protokoll (från referens)

Cellanalys:

[1]
  • Cellinjer

    HUVECs

  • Koncentrationer

    1 μM

  • Inkubationstid

    30 min

  • Metod

    After pretreatment of HUVECs without or with reparixin (1 μM) for 30 min, cells were treated with or without Ang II (100 nmol/l) or CXCL8 (100 ng/ml) for 2 h. Total RNA was then isolated, and real-time PCR was performed.
Djurstudie:

[1]
  • Djurmodeller

    SHR rats

  • Doseringar

    5 mg/kg

  • Administrering

    s.c.

Referenser

  • https://pubmed.ncbi.nlm.nih.gov/21212529/
  • https://pubmed.ncbi.nlm.nih.gov/18587419/
  • https://pubmed.ncbi.nlm.nih.gov/15282370/

Sellecks Reparixin (Repertaxin) Har citerats av 29 Publikationer

Tryptophan 2,3-dioxygenase 2 controls M2 macrophages polarization to promote esophageal squamous cell carcinoma progression via AKT/GSK3β/IL-8 signaling pathway [ Acta Pharmaceutica Sinica B, September 2021, 2835-2849] PubMed: 34589400
NMI induces chemokine release and recruits neutrophils through the activation of NF-κB pathway [ bioRxiv, September 18, 2024, nan]
TRIM26 alleviates fatal immunopathology by regulating inflammatory neutrophil infiltration during Candida infection [ PLoS Pathogens, January 2, 2024, e1011902] PubMed: 38166150
HER2 overexpression triggers the IL-8 to promote arsenic-induced EMT and stem cell-like phenotypes in human bladder epithelial cells [ Ecotoxicology and Environmental Safety, January 15, 2021, 111693] PubMed: 33396024
Bronchial epithelial transcriptomics and experimental validation reveal asthma severity-related neutrophilc signatures and potential treatments [ Communications Biology, February 2024, 181] PubMed: 38351296
Immunothrombolytic monocyte-neutrophil axes dominate the single-cell landscape of human thrombosis and correlate with thrombus resolution [ Immunity, 2025, S1074-7613(25)00139-6] PubMed: 40280129
Harnessing the FGFR2/NF2/YAP signaling-dependent necroptosis to develop an FGFR2/IL-8 dual blockade therapeutic strategy [ Nat Commun, 2025, 16(1):4128] PubMed: 40319089
Nucleus-translocated glucokinase functions as a protein kinase to phosphorylate TAZ and promote tumour growth [ Nat Commun, 2025, 16(1):7156] PubMed: 40759645
Induction of cell death by the CXCR2 antagonist SB225002 in colorectal cancer and stromal cells [ Biomed Pharmacother, 2025, 188:118203] PubMed: 40412356
Chromosomal instability shapes the tumor microenvironment of esophageal adenocarcinoma via a cGAS-chemokine-myeloid axis [ bioRxiv, 2025, 2025.05.06.652454] PubMed: 40654626

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