Reparixin

SKU: orb1303100

Description

Reparixin is a potent small molecule dual CXCR1/CXCR2 antagonist, exhibiting strong inhibition of CXCR1-mediated chemotaxis (IC50=1 nM) and weaker activity against CXCR2 (IC50=100 nM). It is widely used in research to investigate the role of IL-8 signaling in inflammation, cancer metastasis, and ischemia-reperfusion injury in both cellular and animal models.

Research Area

Cancer Biology

Key Properties

• CAS Number: 266359-83-5
• MW: 283.39
• Purity: >98%
• Formula: C₁₄H₂₁NO₃S
• SMILES: CC(C)Cc1ccc(cc1)[C@@H](C)C(=O)NS(C)(=O)=O
• Target: GPCR
• Solubility: Soluble in DMSO (up to 100 mg/ml) or in Ethanol up to 25 mg/ml)

Bioactivity

• Target IC50:
  CXCR1:1 nM|CXCR2:100 nM|CXCR1 (Ile43Val):80 nM (in L1.2 cells)|CXCR1 (wild-type):5.6 nM (in L1.2 cells)
• Cell Research:
  L1.2 Cell suspension (1.5-3×106 cells/mL) is incubated at 37°C for 15 min in the presence of vehicle or of Reparixin (1 nM-1 μM) and next seeded in triplicates in the upper compartment of the chemotactic chamber. Different agonists are seeded in the lower compartment of the chamber at the following concentrations: 1 nM CXCL8, 0.03 nM fMLP, 10 nM CXCL1, 2.5 nM CCL2, 30 nM C5a. The chemotactic chamber is incubated at 37°C in air with 5% CO2 for 45 min (human PMNs) or 2 h (monocytes). At the end of incubation, the filter is removed, fixed, and stained and five oil immersion fields at high magnification (100×) are counted for each migration well after sample coding. L1.2 migration is evaluated using 5 μM pore size Transwell filters.
• Animal Research:
  C57BL/6J mice (8-10 weeks old/20-25 g) are used. The subcutaneous administration of Reparixin (30 mg/kg) is performed 60 minutes before cerebral ischemia induction. The animals are divided into the following three experimental groups: Sham (i.e., the group in which the arteries are visualized, but there is no occlusion of the middle cerebral artery), Vehicle (i.e., the group pre-treated with the vehicle, phosphate buffer solution, 60 minutes before MCAo) and Reparixin (i.e., the group pre-treated with the drug 60 minutes before MCAo). To evaluate neurological signs secondary to MCAo, the animals are assessed with the SHIRPA battery 24 h after reperfusion.

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

DF 1681Y; Repertaxin

Compound Identifiers

PubChem CID

9838712