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Submit ReviewBMS CCR2 22 is a high affinity CCR2 chemokine receptor antagonist (IC50 = 5.1 nM). Displays potent functional antagonism, IC50 values are 1 and 18 nM for chemotaxis and antagonism of calcium flux respectively. Selective over CCR3.
BMS CCR2 22 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Antiviral Library. Find out more about compound libraries available from Tocris.
M. Wt | 593.66 |
Formula | C28H34F3N5O4S |
Storage | Store at +4°C |
Purity | ≥98% (HPLC) |
CAS Number | 445479-97-0 |
PubChem ID | 24801690 |
InChI Key | IBPXYDUJQWENPM-XZOQPEGZSA-N |
Smiles | O=C(N[C@@H]2CCCC[C@@H]2NC(CNC(C3=C(NC(NC(C)C)=O)C=CC(C(F)(F)F)=C3)=O)=O)C1=CC=C(SC)C=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.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 59.37 | 100 | |
ethanol | 5.94 | 10 |
The following data is based on the product molecular weight 593.66. 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 |
---|---|---|---|
1 mM | 1.68 mL | 8.42 mL | 16.84 mL |
5 mM | 0.34 mL | 1.68 mL | 3.37 mL |
10 mM | 0.17 mL | 0.84 mL | 1.68 mL |
50 mM | 0.03 mL | 0.17 mL | 0.34 mL |
References are publications that support the biological activity of the product.
Cherney et al (2008) Discovery of disubstituted cyclohexanes as a new class of CC chemokine receptor 2 antagonists. J.Med.Chem. 51 721 PMID: 18232650
You et al (2010) CCR2 receptor ligands inhibit Cav3.2 T-type calcium channels. Mol.Pharmacol. 77 211 PMID: 19864434
If you know of a relevant reference for BMS CCR2 22, please let us know.
Keywords: BMS CCR2 22, BMS CCR2 22 supplier, High, affinity, potent, CCR2, antagonists, Chemokine, Receptors, BMSCCR222, CC, 3129, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for BMS CCR2 22 include:
Volpe et al (2012) CCR2 acts as scavenger for CCL2 during monocyte chemotaxis. PLoS One 7 e37208 PMID: 22615942
Barzilai et al (2016) M-sec regulates polarized secretion of inflammatory endothelial chemokines and facilitates CCL2-mediated lymphocyte transendothelial migration. J Leukoc Biol 99 1045 PMID: 26701136
Wang et al (2022) Regulation of CCL2 by EZH2 affects tumor-associated macrophages polarization and infiltration in breast cancer. Cell Death Dis 13 748 PMID: 36038549
Wang et al (2018) Effect of CCR2 inhibitor-loaded lipid micelles on inflammatory cell migration and cardiac function after myocardial infarction. Int J Nanomedicine 13 6441 PMID: 30410330
Do you know of a great paper that uses BMS CCR2 22 from Tocris? Please let us know.
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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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Rheumatoid arthritis (RA) is a chronic destructive inflammatory autoimmune disease that results from a breakdown in immune tolerance, for reasons that are as yet unknown. This poster summarizes the pathology of RA and the inflammatory processes involved, as well as describing some of the epigenetic modifications associated with the disease and the potential for targeting these changes in the discovery of new treatments.