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Submit ReviewRS 504393
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)
Biological Activity for RS 504393
RS 504393 is an 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 for RS 504393
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for RS 504393
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 4.17 | 10 |
Preparing Stock Solutions for RS 504393
The following data is based on the product molecular weight 417.5. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 23.95 mL | 119.76 mL | 239.52 mL |
| 0.5 mM | 4.79 mL | 23.95 mL | 47.9 mL |
| 1 mM | 2.4 mL | 11.98 mL | 23.95 mL |
| 5 mM | 0.48 mL | 2.4 mL | 4.79 mL |
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Product Datasheets for RS 504393
References for RS 504393
References are publications that support the biological activity of the product.
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
If you know of a relevant reference for RS 504393, please let us know.
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Keywords: RS 504393, RS 504393 supplier, selective, CCR2, chemokine, receptor, antagonists, CXCR, Chemokine, Receptors, RS504393, CC, 2517, Tocris Bioscience
15 Citations for RS 504393
Citations are publications that use Tocris products. Selected citations for RS 504393 include:
Arendt et al (2013) Obesity promotes breast cancer by CCL2-mediated macrophage recruitment and angiogenesis. J Biol Chem 73 6080 PMID: 23959857
Tong et al (2018) Concomitant type I IFN and M-CSF signaling reprograms monocyte differentiation and drives pro-tumoral arginase production. EBioMedicine PMID: 30528455
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
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
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
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
Kwiatkowski et al (2017) The RS504393 Influences the Level of Nociceptive Factors and Enhances Opioid Analgesic Potency in Neuropathic Rats. J Neuroimmune Pharmacol PMID: 28337574
Linde (2018) Macrophages orchestrate breast cancer early dissemination and metastasis. Nat Commun 9 21 PMID: 29295986
Kim et al (2014) IL-33-induced hematopoietic stem and progenitor cell mobilization depends upon CCR2. J Immunol 193 3792 PMID: 25143444
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
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
Do you know of a great paper that uses RS 504393 from Tocris? Please let us know.
Reviews for RS 504393
Average Rating: 5 (Based on 1 Review.)
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Used for Migration assays.
By
Anonymous on 07/01/2020
Assay Type: In Vitro
Species: Human
Cell Line/Tissue: A549 or MDAMB231
Receptor antagonists (SB225002: for CXCR2, AMD3465: for CXCR4, RS504393: for CCR2 and Maraviroc: for CCR5) at 10 μM
We ordered this product, combining with another inhibitor, to confirm the migration.To confirm that tested product induces migration, we also screen all MAPK inhibitors and MIF receptor antagonists
Literature in this Area
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