Reparixin L-lysine salt

SKU: orb1218244

Description

Reparixin L-lysine salt is an allosteric chemokine receptor 1/2 (CXCR1/2) activation inhibitor.

Images & Validation

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Key Properties

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CAS Number	266359-93-7
MW	429.57
Purity	>98% (HPLC)
Formula	C₂₀H₃₅N₃O₅S
SMILES	N[C@@H](CCCCN)C(O)=O.O=C(NS(=O)(C)=O)[C@@H](C)C1=CC=C(CC(C)C)C=C1
Target	CXCR
Solubility	H2O: 99 mg/mL (230.46 mM; Need ultrasonic); DMSO: 99 mg/mL (230.46 mM; Need ultrasonic)

Bioactivity

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In Vivo

The pharmacokinetics and metabolism of Reparixin are investigated in rats and dogs after intravenous administration of [14C]-Reparixin L-lysine salt. Plasma protein binding of Reparixin is >99% in the laboratory animals and humans up to 50 μg/mL, but lower at higher concentrations. Although radioactivity is rapidly distributed into rat tissues, Vss is low (about 0.15 L/kg) in both rat and dog. Nevertheless, Reparixin is more rapidly eliminated in rats (t1/2~0.5 h) than in dogs (t1/2~10 h).

In Vitro

Reparixin is a potent functional inhibitor of CXCL8-induced 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. 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). Reparixin is a non-competitive allosteric inhibitor of IL-8 receptors with a 400-fold higher efficacy in inhibiting CXCR1 activity than CXCR2.

Storage & Handling

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Storage	Storage temperature: -20°C. Stability: ≥ 2 years
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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Repertaxin L-lysine salt

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Gene Symbol

CXCR

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