RS 504393

Cat. No. 2517

RS 504393 C25H27N3O3 [300816-15-3]

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Chemical Name: 6-Methyl-1'-[2-(5-methyl-2-phenyl-4-oxazolyl)ethyl]-spiro[4H-3,1-benzoxazine-4,4'-piperidin]-2(1H)-one

Biological Activity

Extremely selective CCR2 chemokine receptor antagonist (IC50 values are 98 nM and > 100 μM for inhibition of human recombinant CCR2b and CCR1 receptors respectively). Inhibits MCP-1 chemotaxis (IC50 = 330 nM) and ischemia-reperfusion injury in kidneys.

Technical Data

Soluble to 10 mM in DMSO
>99 %
Store at +4°C

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Datasheet

Certificate of Analysis / Product Datasheet
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References are publications that support the products' biological activity.

Kitagawa et al (2004) Blockade of CCR2 ameliorates progressive fibrosis in kidney. Am.J.Pathol. 165 237. PMID: 15215179.

Furuichi et al (2003) CCR2 signaling contributes to ischemia-reperfusion injury in kidney. J.Am.Soc.Nephrol. 14 2503. PMID: 14514728.

Mirzadegan et al (2000) Identification of the binding site for a novel class of CCR2b chemokine receptor antagonists. J.Biol.Chem. 275 25562. PMID: 10770925.

If you know of a relevant reference for RS 504393 please let us know.

Citations are publications that use Tocris products. Selected citations for RS 504393 include:

Ayoub et al (2015) Functional Interaction between Angiotensin II Receptor Type 1 and Chemokine (C-C Motif) Receptor 2 with Implications for Chronic Kidney Disease. PLoS One 10 e0119803. PMID: 25807547.

Lourenco et al (2015) Macrophage migration inhibitory factor-CXCR4 is the dominant chemotactic axis in human mesenchymal stem cell recruitment to tumors. J Immunol 194 3463. PMID: 25712213.

Lu et al (2015) Inhibiting the mobilization of Ly6C(high) monocytes after acute myocardial infarction enhances the efficiency of mesenchymal stromal cell transplantation and curbs myocardial remodeling. J Neurosci 7 587. PMID: 26045897.

Matsubara et al (2015) Secreted ectodomain of sialic acid-binding Ig-like lectin-9 and monocyte chemoattractant protein-1 promote recovery after rat spinal cord injury by altering macrophage polarity. Cancer Res 35 2452. PMID: 25673840.

Mazumdar et al (2015) CoREST1 Promotes Tumor Formation and Tumor Stroma Interactions in a Mouse Model of Breast Cancer. PLoS One 10 e0121281. PMID: 25793264.

Kim et al (2014) IL-33-induced hematopoietic stem and progenitor cell mobilization depends upon CCR2. J Immunol 193 3792. PMID: 25143444.

Arendt et al (2013) Obesity promotes breast cancer by CCL2-mediated macrophage recruitment and angiogenesis. J Biol Chem 73 6080. PMID: 23959857.

Arms et al (2013) Expression and function of CCL2/CCR2 in rat micturition reflexes and somatic sensitivity with urinary bladder inflammation. Am J Physiol Renal Physiol 305 F111. PMID: 23594826.

Miller et al (2012) CCR2 chemokine receptor signaling mediates pain in experimental osteoarthritis. Proc Natl Acad Sci U S A 109 20602. PMID: 23185004.

Zhang et al (2012) Chemokine CCL2 and its receptor CCR2 in the medullary dorsal horn are involved in trigeminal neuropathic pain. J Neuroinflammation 9 136. PMID: 22721162.

Simonson and Ismail-Beigi (2011) Endothelin-1 increases collagen accumulation in renal mesangial cells by stimulating a chemokine and cytokine autocrine signaling loop. Br J Pharmacol 286 11003. PMID: 21169360.

Yang et al (2009) Inhibition of the chemokine (C-C motif) ligand 2/chemokine (C-C motif) receptor 2 pathway attenuates hyperglycaemia and inflammation in a mouse model of hepatic steatosis and lipoatrophy. Diabetologia 52 972. PMID: 19277603.

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Keywords: RS 504393, supplier, selective, CCR2, chemokine, receptor, antagonists, CXCR, Chemokine, Receptors, RS504393, Tocris Bioscience, Chemokine CC Receptor Antagonist products

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