1. GPCR/G Protein
    Immunology/Inflammation
  2. CXCR
  3. Reparixin L-lysine salt

Reparixin L-lysine salt (Synonyms: Repertaxin L-lysine salt)

Cat. No.: HY-15252 Purity: 99.97% ee.: 99.49%
Handling Instructions

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

For research use only. We do not sell to patients.

Reparixin L-lysine salt Chemical Structure

Reparixin L-lysine salt Chemical Structure

CAS No. : 266359-93-7

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Customer Review

Based on 30 publication(s) in Google Scholar

Other Forms of Reparixin L-lysine salt:

Top Publications Citing Use of Products

    Reparixin L-lysine salt purchased from MCE. Usage Cited in: J Gastroenterol Hepatol. 2018 Feb;33(2):431-442.

    The effects of TRAF2 overexpression with or without Reparixin (100 nM), or BAY 11-7082 (30 μM) on the migration and invasion of AGS cell are examined by transwell assay.

    Reparixin L-lysine salt purchased from MCE. Usage Cited in: Oncogenesis. 2016 Jun 13;5(6):e234.

    The effects of Reparixin (100 nM) on the migration of OLFM4-depleted gastric cancer cells are detected by transwell assay.

    Reparixin L-lysine salt purchased from MCE. Usage Cited in: Oncotarget. 2017 Jul 21;8(36):60210-60222.

    Migration assay of MDA-MB-231 cells treated 0.1 uM of Reparixin in CM from fibroblasts or macrophages with TCM of MDA-MB-231 cells using the Oris Cell migration kit.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

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

    IC50 & Target

    CXCR1wt

    5.6 nM (IC50, in L1.2 cells)

    CXCR1Ile43Val

    80 nM (IC50, in L1.2 cells)

    CXCR1

    1 nM (IC50, in cells)

    CXCR2

    ∼100 nM (IC50, in cells)

    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)[1]. Reparixin is a non-competitive allosteric inhibitor of IL-8 receptors with a 400-fold higher efficacy in inhibiting CXCR1 activity than CXCR2[2].

    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)[3].

    Clinical Trial
    Molecular Weight

    429.57

    Formula

    C₂₀H₃₅N₃O₅S

    CAS No.

    266359-93-7

    SMILES

    N[[email protected]@H](CCCCN)C(O)=O.CS(=O)(NC([[email protected]@H](C1=CC=C(CC(C)C)C=C1)C)=O)=O

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    H2O : ≥ 200 mg/mL (465.58 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.3279 mL 11.6395 mL 23.2791 mL
    5 mM 0.4656 mL 2.3279 mL 4.6558 mL
    10 mM 0.2328 mL 1.1640 mL 2.3279 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Reparixin L-lysine salt is prepared in saline[4].

    References
    Cell Assay
    [1]

    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[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [3]

    Rats and Dogs[3]
    Male and female Sprague-Dawley CD (albino) rats and male Lister Hooded (partially pigmented) rats are used. Male and female beagle Dogs (age about 15 months, bodyweight range 8.3-9.4 kg at the time of dosing) are used. Rats and Dogs are dosed i.v. with repurified [14C]-Reparixin free acid and an equivalent quantity of L-lysine suitably radiodiluted with Reparixin L-lysine salt in a solution of sterile isotonic (0.9%, w/v) saline. Rats are dosed with a solution of total drug concentration 9 mg/mL at a dose volume of 5 mL/kg (30 mg free Reparixin /kg) by bolus injection into a caudal vein. Dogs are dosed with a solution of total drug concentration 100 mg/mL at a dose volume of 0.5 mL/kg (33 mg free Reparixin/kg) by bolus injection into a superficial forelimb vein.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References

    Purity: 99.97% ee.: 99.49%

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    Keywords:

    ReparixinRepertaxinCXCRCXC chemokine receptorsC-X-C motif chemokine receptorsInhibitorinhibitorinhibit

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    Product name:
    Reparixin L-lysine salt
    Cat. No.:
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