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

Navarixin (Synonyms: SCH 527123; MK-7123)

Cat. No.: HY-10198 Purity: 98.62%
Handling Instructions

Navarixine (SCH 527123) est un antagoniste des CXCR1 et CXCR2 qui est puissant, allostérique et oralement actif, avec Kd valeurs de 41 nM pour cynomolgus CXCR1 et 0,20 nM, 0,20 nM, 0,08 nM pour souris, rat et cynomolgus monkey CXCR2, respectivement.

Navarixin (SCH 527123) is a potent, allosteric and orally active antagonist of both CXCR1 and CXCR2, with Kd values of 41 nM for cynomolgus CXCR1 and 0.20 nM, 0.20 nM, 0.08 nM for mouse, rat and cynomolgus monkey CXCR2, respectivelly.

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

Navarixin Chemical Structure

Navarixin Chemical Structure

CAS No. : 473727-83-2

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10 mg USD 150 In-stock
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50 mg USD 450 In-stock
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100 mg USD 750 In-stock
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Based on 12 publication(s) in Google Scholar

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Description

Navarixin (SCH 527123) is a potent, allosteric and orally active antagonist of both CXCR1 and CXCR2, with Kd values of 41 nM for cynomolgus CXCR1 and 0.20 nM, 0.20 nM, 0.08 nM for mouse, rat and cynomolgus monkey CXCR2, respectivelly[1][2].

IC50 & Target

125I-CXCL8-CXCR2

0.97 nM (IC50)

Cynomolgus CXCR2

0.08 nM (Kd)

Mouse CXCR2

0.2 nM (Kd)

Rat CXCR2

0.2 nM (Kd)

125I-CXCL8-CXCR1

43 nM (IC50)

Cynomolgus CXCR1

41 nM (Kd)

In Vitro

Navarixin is a potent, allosteric antagonist of both CXCR1 and CXCR2, with Kd values of 41 nM for cynomolgus CXCR1 and 0.20 nM, 0.20 nM, 0.08 nM for mouse, rat and cynomolgus monkey CXCR2, respectivelly[1]. Navarixin (1 nM) reduces CXCL8 potency in stimulating Ba/F3-hCXCR2 chemotaxis. Navarixin (3 nM) significantly inhibits the potency and efficacy of CXCL1-induced neutrophils (PMN) chemotaxis. Navarixin (300 nM) significantly decreases chemokine potency and slightly decreases maximal cell movement for Ba/F3-CXCR1 cells[2]. Navarixin (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].

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

In Vivo

Navarixin (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, Navarixin (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[1].

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

Clinical Trial
Molecular Weight

397.42

Formula

C₂₁H₂₃N₃O₅

CAS No.

473727-83-2

SMILES

O=C1C(C(NC2=CC=CC(C(N(C)C)=O)=C2O)=C1N[[email protected]](CC)C3=CC=C(O3)C)=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: 

DMSO : ≥ 50 mg/mL (125.81 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent 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.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.29 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (6.29 mM); Suspended solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.29 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[2]

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 Navarixin (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[2].

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

Animal Administration
[1]

Mice[1]
Male BALB/c mice weighing between 20 and 25 g are used. Control mice receive intranasal injection of 50 μL of isotonic (0.9%) saline. Navarixin (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 Navarixin or vehicle are given[1].
Rats[1]
Male Sprague-Dawley rats (200 g) are used. Control animals receive 100 μL of isotonic saline. Navarixin (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 Navarixin or vehicle is given in these experiments[1].

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

References
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Keywords:

NavarixinSCH 527123 MK-7123SCH527123SCH-527123MK7123MK 7123MK-7123CXCRCXC chemokine receptorsC-X-C motif chemokine receptorsInhibitorinhibitorinhibit

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