RS 504393

Pricing Availability Delivery Time Qty
Cat.No. 2517 - RS 504393 | C25H27N3O3 | CAS No. 300816-15-3
Description: Highly selective CCR2 chemokine receptor antagonist
Chemical Name: 6-Methyl-1'-[2-(5-methyl-2-phenyl-4-oxazolyl)ethyl]-spiro[4H-3,1-benzoxazine-4,4'-piperidin]-2(1H)-one
Purity: ≥99% (HPLC)
Datasheet
Citations (12)
Literature

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

M. Wt 417.5
Formula C25H27N3O3
Storage Store at +4°C
Purity ≥99% (HPLC)
CAS Number 300816-15-3
PubChem ID 9953769
InChI Key ODNICNWASXKNNQ-UHFFFAOYSA-N
Smiles CC1=C(CCN2CCC3(CC2)OC(=O)NC2=C3C=C(C)C=C2)N=C(O1)C1=CC=CC=C1

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 4.17 10

Preparing Stock Solutions

The following data is based on the product molecular weight 417.5. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.4 mL 11.98 mL 23.95 mL
5 mM 0.48 mL 2.4 mL 4.79 mL
10 mM 0.24 mL 1.2 mL 2.4 mL
50 mM 0.05 mL 0.24 mL 0.48 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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

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

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


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

12 Citations for RS 504393

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

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

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

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

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

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

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

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

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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