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Navarixin (SCH-527123) CXCR1/2 Antagonist

Cat.No.S8506

Navarixin (SCH-527123, MK-7123, PS-291822) is a potent, orally bioavailable CXCR2/CXCR1 antagonist with IC50 values of 2.6 nM and 36 nM, respectively.
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Quality Control

Batch: Purity: 99.68%
99.68

Solubility

In vitro
Batch:

DMSO : 79 mg/mL (198.78 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 79 mg/mL

Water : Insoluble

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Mass Concentration Volume Molecular Weight
Dilution Calculator Molecular Weight Calculator

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

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%
% Tween 80
% ddH2O
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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight 397.42 Formula

C21H23N3O5

Storage (From the date of receipt) 3 years -20°C powder
CAS No. 473727-83-2 -- Storage of Stock Solutions

Synonyms MK-7123, PS-291822 SMILES CCC(C1=CC=C(O1)C)NC2=C(C(=O)C2=O)NC3=CC=CC(=C3O)C(=O)N(C)C

Read more about storage stability stock solution CAS number SMILES

Mechanism of Action

Targets/IC50/Ki
CXCR2
(Cell-free assay)
2.6 nM
CXCR1
(Cell-free assay)
36 nM
In vitro

Navarixin (SCH-527123, MK-7123, PS-291822) is a potent, orally bioavailable CXCR2/CXCR1 antagonist with IC50 values of 2.6 nM and 36 nM, respectively.

In vivo

SCH52712, a novel, orally active CXCR1/2 receptor antagonist, inhibits neutrophil recruitment, mucus production, and goblet cell hyperplasia in animal models of pulmonary inflammation.

References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-08-28)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03473925 COMPLETED
Solid Tumors; Non-small Cell Lung Cancer; Castration Resistant Prostate Cancer; Microsatellite Stable Colorectal Cancer
Merck Sharp & Dohme LLC
2018-04-10 PHASE2
NCT01006161 WITHDRAWN
Asthma
Merck Sharp & Dohme LLC
2010-01 PHASE2
NCT01006616 TERMINATED
COPD
Merck Sharp & Dohme LLC
2009-10-01 PHASE2
NCT01068145 TERMINATED
Chronic Obstructive Pulmonary Disease
Merck Sharp & Dohme LLC
2010-02 PHASE1
NCT01068145 Terminated
Chronic Obstructive Pulmonary Disease
Merck Sharp & Dohme LLC
2010-02 Phase 1
NCT00688467 COMPLETED
Asthma
Merck Sharp & Dohme LLC
2008-06-01 PHASE2

Read more about Clinical Trials

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