Reparixin, CXCR1/2 allosteric antagonist (TBI2527)

Description

Product Details

Formal Name: αR-Methyl-4-(2-methylpropyl)-N-(methylsulfonyl)-benzeneacetamide

Alternate Names: DF 1681Y; Repertaxin

Molecular Formula: C₁₄H₂₁NO₃S

Formula Weight: 283.39

CAS Number: 266359-83-5

Purity: >98%

Formulation: powder

Solubility: Soluble in DMSO (up to 100 mg/ml) or in Ethanol up to 25 mg/ml)

Storage: -20°C

Stability: ≥ 1 year.

Applications

CXCR1/2 allosteric antagonist

Functions

Reparixin is a noncompetitive allosteric inhibitor of IL-8 (CXCL8) activation of CXCR1 and CXCR2 chemokine receptors (IC50 = 1 and 100 nM, respectively). It blocks a number of activities related to IL-8 signaling, including leukocyte recruitment (IC50 = 1 nM) without affecting receptor activation induced by other CXCR1 and CXCR2 agonists. In spontaneously hypertensive rats, 5 mg/kg reparixin administered daily for three weeks was shown to reduce blood pressure by inhibiting hypertension-related mediators. It attenuates inflammatory responses and promotes recovery of function after traumatic lesion to the spinal cord. Reparixin blockade (100 nM) of CXCR1 has also been used to deplete a cancer stem cell population in human breast cancer cell lines in vitro.

Application Procedures

First dissolved in DMSO (up to 100 mg/ml) or in Ethanol up to 25 mg/ml), then diluted to aqueous buffer. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.