Reparixin L-lysine salt

SKU: orb1309168

Description

Repertaxin L-lysine salt is a small molecule, allosteric inhibitor targeting the CXCR1 and CXCR2 chemokine receptors. It is widely used in research to investigate the role of these receptors in inflammatory diseases and cancer metastasis, with applications in both in vitro cellular assays and in vivo animal models.

Research Area

Cell Biology, Immunology & Inflammation, Pharmacology & Drug Discovery

Images & Validation

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Key Properties

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CAS Number	266359-93-7
MW	429.57
Purity	99.00%
Formula	C₂₀H₃₅N₃O₅S
SMILES	NCCCC[C@H](N)C(O)=O.CC(C)Cc1ccc(cc1)[C@@H](C)C(=O)NS(C)(=O)=O
Target	CXCR
Solubility	DMSO:99 mg/mL (230.46 mM);H2O:99 mg/mL (230.46 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (7.68 mM)

Bioactivity

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Target IC50	CXCR2:100 nM (in cells)\|CXCR1:1 nM (in cells)\|CXCR1:5.6 nM (CXCR1wt, in L1.2 cells)\|CXCR1:80 nM (CXCR1Ile43Val; in L1.2 cells)
In Vivo	The pharmacokinetics and metabolism of Reparixin were investigated in rats and dogs following the intravenous administration of [14C]-Reparixin L-lysine salt. Plasma protein binding of Reparixin is >99% in both laboratory animals and humans up to 50 μg/mL, but decreases at higher concentrations. Radioactivity rapidly distributes into rat tissues, yet the volume of distribution at steady state (Vss) is low (approximately 0.15 L/kg) in both rats and dogs. Reparixin is eliminated more rapidly in rats (t1/2~0.5 h) than in dogs (t1/2~10 h). Read more...
In Vitro	Reparixin is a potent CXCL8-induced inhibitor biological activities on human PMNs, with a marked selectivity (around 400-fold) for CXCR1, as shown in specific experiments on CXCR1/L1.2 and CXCR2/L1.2 transfected cells and on human PMNs.Reparixin is a non-competitive allosteric inhibitor of IL-8 receptors with a 400-fold higher efficacy in inhibiting CXCR1 activity than CXCR2. The efficacy of Reparixin is significantly lower in L1.2 cells expressing Ile43Val CXCR1 mutant (IC50 values of 5.6 nM and 80 nM for CXCR1 wt and CXCR1 Ile43Val, respectively). Read more...

Storage & Handling

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Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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CXCR, CXCR1, CXCR1Ile43Val, CXCR1wt, CXCR2, CXC chemokine receptors, inhibit, Inhibitor, Repertaxin, Repertaxin L-lysine, Repertaxin L-lysine salt, Reparixin, Reparixin L lysine salt, Reparixin L-lysine, Reparixin Llysine salt

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Compound Identifiers

PubChem CID

9932389 ↗

Key Properties

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No computed properties available.

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