SCH 527123 - CAS 473727-83-2
Catalog number: 473727-83-2
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C21H23N3O5
Molecular Weight:
397.42
COA:
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Targets:
CXCR
Description:
A potent antagonist of both CXCR1 and CXCR2 with IC50 of 42 nM and 3 nM, respectively.
Brife Description:
A potent antagonist of both CXCR1 and CXCR2 with IC50 of 42 nM and 3 nM, respectively.
Appearance:
Light yellow to yellow solid
Synonyms:
2-hydroxy-N,N-dimethyl-3-(2-((1-(5-methylfuran-2-yl)propyl)amino)-3,4-dioxocyclobut-1-enylamino)benzamide; SCH527123; SCH-527123; SCH 527123; MK-7123; MK7123; MK 7123; PS291822; PS-291822; PS 291822; Navarixin monohydrate; Navarixin
Solubility:
Soluble to 100 mM in DMSO
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
MSDS:
Inquire
Quality Standard:
In-house
Quantity:
Grams-Kilos
Boiling Point:
548.67 °C at 760 mmHg
Melting Point:
118-120 ºC
InChIKey:
RXIUEIPPLAFSDF-CYBMUJFWSA-N
InChI:
1S/C21H23N3O5/c1-5-13(15-10-9-11(2)29-15)22-16-17(20(27)19(16)26)23-14-8-6-7-12(18(14)25)21(28)24(3)4/h6-10,13,22-23,25H,5H2,1-4H3/t13-/m1/s1
Canonical SMILES:
CCC(C1=CC=C(O1)C)NC2=C(C(=O)C2=O)NC3=CC=CC(=C3O)C(=O)N(C)C
1.LPS challenge in healthy subjects: an investigation of neutrophil chemotaxis mechanisms involving CXCR1 and CXCR2.
Aul R1, Patel S, Summerhill S, Kilty I, Plumb J, Singh D. Int Immunopharmacol. 2012 Jul;13(3):225-31. doi: 10.1016/j.intimp.2012.04.008. Epub 2012 May 2.
LPS inhalation was used to investigate whether sputum supernatant post-LPS challenge increases neutrophil chemotactic activity and to elucidate the role of CXCR1/CXCR2 signalling in this process. 14 healthy non-smoking subjects inhaled 30μg of LPS. Sputum was induced at baseline, 6 and 24h post-LPS challenge. Differential cell counts were determined and supernatants CXCL8, CXCL1, IL-6 and CCL2 levels measured. Peripheral blood neutrophils obtained from healthy volunteers were used for chemotaxis experiments using sputum supernatant. To delineate signalling mechanisms, the effects of a CXCR2/CXCR1 (dual) antagonist (Sch527123) and a CXCR2 specific antagonist (SB656933) were tested. LPS inhalation significantly increased sputum neutrophil counts from 45.3% to 76.7% and 69.3% at 6 and 24h respectively. LPS increased CXCL8, IL-6 and CCL2 levels but not CXCL1. Neutrophil chemotaxis significantly increased (2.7 fold) at 24h compared to baseline.
2.CXCR2 Antagonist MK-7123. A Phase 2 Proof-of-Concept Trial for Chronic Obstructive Pulmonary Disease.
Rennard SI1, Dale DC, Donohue JF, Kanniess F, Magnussen H, Sutherland ER, Watz H, Lu S, Stryszak P, Rosenberg E, Staudinger H. Am J Respir Crit Care Med. 2015 May 1;191(9):1001-11. doi: 10.1164/rccm.201405-0992OC.
RATIONALE: An antagonist (MK-7123) of the cytokine receptor CXCR2 reduces neutrophil chemotaxis and thus may alleviate airway inflammation in chronic obstructive pulmonary disease (COPD).
3.Humoral immunity and delayed-type hypersensitivity in healthy subjects treated for 30 days with MK-7123, a selective CXCR2 antagonist.
Seiberling M1, Kamtchoua T, Stryszak P, Ma X, Langdon RB, Khalilieh S. Int Immunopharmacol. 2013 Oct;17(2):178-83. doi: 10.1016/j.intimp.2013.05.029. Epub 2013 Jun 19.
Antagonism of the chemokine receptor CXCR2 inhibits neutrophil trafficking and may thus be therapeutic in patients with chronic obstructive pulmonary disease and other lung disorders in which there is substantial infiltration by neutrophils. Here, we report the findings from a randomized, placebo-controlled, double-blind clinical trial of the small-molecule CXCR2 antagonist MK-7123 (formerly SCH 527123) that evaluated potential downstream effects of CXCR2 antagonism on immunogenic competency (B cell antibody response) in the adaptive immune system and delayed-type hypersensitivity (DTH) in healthy subjects (ages 34-65 years) dosed once daily for 30 days either with 30 mg MK-7123 (n=24) or placebo (n=7). Eligible subjects were seronegative for anti-hepatitis A virus (HAV) immunoglobulin G (IgG) and positive for DTH response to intradermal injection of Candida albicans antigen at screening. Subjects were vaccinated for HAV on treatment Day 2.
4.The CXCL8/IL-8 chemokine family and its receptors in inflammatory diseases.
Russo RC1, Garcia CC, Teixeira MM, Amaral FA. Expert Rev Clin Immunol. 2014 May;10(5):593-619. doi: 10.1586/1744666X.2014.894886. Epub 2014 Mar 29.
Chemokines are small proteins that control several tissue functions, including cell recruitment and activation under homeostatic and inflammatory conditions. CXCL8 (interleukin-8) is a member of the chemokine family that acts on CXCR1 and CXCR2 receptors. CXCL1, CXCL2, CXCL3, CXCL5, CXCL6, and CXCL7 are also ELR+ chemokine members that bind to these receptors, especially CXCR2. The majority of studies on the biology of CXCL8 and their receptors have been performed in polymorphonuclear leukocytes. However, many other cells express CXCR1/CXCR2, including epithelial, endothelial, fibroblasts and neurons, contributing to the biological effects of CXCL8. There is substantial amount of experimental data suggesting that CXCL8 and receptors contribute to elimination of pathogens, but may also contribute significantly to disease-associated processes, including tissue injury, fibrosis, angiogenesis and tumorigenesis. Here, we discuss the biology of CXCL8 family and the potential therapeutic use of antagonists or blockers of these molecules in the context of organ-specific diseases.
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Chemical Structure

CAS 473727-83-2 SCH 527123

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