1. GPCR/G Protein
    Immunology/Inflammation
  2. CXCR

SCH 527123 

Cat. No.: HY-10198 Purity: 99.06%
Data Sheet SDS Handling Instructions

SCH 527123 is a potent, allosteric antagonist of both CXCR1 and CXCR2, with IC50 values of 1000 nM and 3-6 nM, respectivelly.

For research use only. We do not sell to patients.
SCH 527123 Chemical Structure

SCH 527123 Chemical Structure

CAS No. : 473727-83-2

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $154 In-stock
5 mg $140 In-stock
10 mg $240 In-stock
50 mg $480 In-stock
100 mg $900 In-stock
200 mg   Get quote  
500 mg   Get quote  

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    SCH 527123 purchased from MCE. Usage Cited in: J Allergy Clin Immunol. 2016 Jul;138(1):114-122.e4.

    A selective CXCR3 receptor antagonist abrogates fibroblast migration to HRV MED (n=6).
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    SCH 527123 is a potent, allosteric antagonist of both CXCR1 and CXCR2, with IC50 values of 1000 nM and 3-6 nM, respectivelly.

    IC50 & Target

    IC50: 1000 nM (CXCR1), 3-6 nM (CXCR2)[2]

    In Vitro

    Sch527123 (1 nM) reduces CXCL8 potency in stimulating Ba/F3-hCXCR2 chemotaxis. Sch527123 (3 nM) significantly inhibits the potency and efficacy of CXCL1-induced neutrophils (PMN) chemotaxis. Sch527123 (300 nM) significantly decreases chemokine potency and slightly decreases maximal cell movement for Ba/F3-CXCR1 cells[1]. SCH-527123 (25 μM) is sufficient to block IL-8-mediated CXCR2 activation in HCT116, E2, Caco2, and IIIe cells, in which phosphorylation of downstream kinases of CXCR2 is reduced in a concentration-dependent manner[3].

    In Vivo

    Sch527123 (0.1-10 mg/kg, p.o.) blocks pulmonary neutrophilia (ED50=1.2 mg/kg) and goblet cell hyperplasia (32-38% inhibition at 1-3 mg/kg) in mice following the intranasal lipopolysaccharide (LPS) administration. In rats, Sch527123 (0.1-3 mg/kg p.o.) suppresses the pulmonary neutrophilia (ED=1.8 mg/kg) and increase in bronchoalveolar lavage (BAL) mucin content (ED50=0.1 mg/kg) induced by intratracheal (i.t.) LPS[2].

    Clinical Trial
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    References
    Preparing Stock Solutions
    Concentration Volume Mass 1 mg 5 mg 10 mg
    1 mM 2.5162 mL 12.5811 mL 25.1623 mL
    5 mM 0.5032 mL 2.5162 mL 5.0325 mL
    10 mM 0.2516 mL 1.2581 mL 2.5162 mL
    Please refer to the solubility information to select the appropriate solvent.
    Kinase Assay
    [1]

    Neutrophils are cultured with 5 mM cytochalasin B with or without Sch527123 at 37°C for 10 min. Agonists are added, and the cells are incubated for an additional 1 h at 37°C. Tetramethylbenzidine substrate is added, and OD450 is read to determine myeloperoxidase activity in the supernatant. Myeloperoxidase release is normalized to total release after the addition of 1% Triton X-100. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Assay
    [1]

    Recombinant cells are resuspended at 1×106/mL in assay buffer (phenol red free-RPMI 1640 supplemented with 2% FBS). Human neutrophils are resuspended at 2 × 106/mL in the same assay buffer containing 5% FBS. CXCL1 binds only CXCR2 with high affinity, whereas CXCL8 binds both CXCR1 and CXCR2 with high affinity. Chemoattractants (30 μL) diluted in assay buffer are dispensed into the bottom wells of disposable microchemotaxis plates, which are then covered with filter. Cells are preincubated with Sch527123 (1-300 nM) in a CO2 incubator for 90 min. Cell aliquots (25 μL) are applied to each spot on the filter. After incubation (90 min for BaF/3 cells and 30 min for PMN in a CO2 incubator), the filters are removed. Migrated cells in the bottom wells are transferred to a Microlite luminometer plate, and 25 μL of ATPlite one-step are added to each well. After incubation at room temperature for 10 min, luminescence intensity is measured using a luminometer. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [2]

    SCH 527123 is suspended in 0.4% methylcellulose vehicle for both mice and rat assay[2].

    Mice[2]
    Male BALB/c mice weighing between 20 and 25 g are anesthetized by intraperitoneal injection of ketamine (100 mg/kg) and xylazine (10 mg/kg), and 50 μL of a 1 mg/mL LPS solution (50 μg/mouse) is instilled into the lungs via the intranasal route of administration. Control mice receive intranasal injection of 50 μL of isotonic (0.9%) saline. Sch527123 (0.1-10 mg/kg, p.o.) is suspended in 0.4% methylcellulose and given orally by gavage 2 h before and 4 h after each intranasal administration of LPS. Control animals receive 0.4% methylcellulose (10 mL/kg). In total, four doses of Sch527123 or vehicle are given.
    Rat[2]
    Male Sprague-Dawley rats (200 g) are anesthetized with 5% isoflurane supplemented with oxygen and receive 100 μLof LPS (100 μg/mL), dissolved in isotonic (0.9%) saline to deliver a dose of 10 μg/rat. Control animals receive 100 μL of isotonic saline. Sch527123 (0.1-3 mg/kg, p.o.) is suspended in 0.4% methylcellulose vehicle and given orally 2 h before the LPS challenge. Control rats receive oral methylcellulose (10 mL/kg). Only one dose of Sch527123 or vehicle is given in these experiments. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    397.42

    Formula

    C₂₁H₂₃N₃O₅

    CAS No.

    473727-83-2

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    10 mM in DMSO

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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    Product Name:
    SCH 527123
    Cat. No.:
    HY-10198
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