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BMS CCR2 22

Catalog #: 3129
4 Citations Datasheet
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3129/10
3129/50
3129/1
BMS CCR2 22 | CAS No. 445479-97-0 | Chemokine Receptor Antagonists
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Description: High affinity, potent CCR2 antagonist

Chemical Name: 2-[(Isopropylaminocarbonyl)amino]-N-[2-[[cis-2-[[4-(methylthio)benzoyl]amino]cyclohexyl]amino]-2-oxoethyl]-5-(trifluoromethyl)benzamide

Purity: ≥98%

Product Details
Citations (4)
Supplemental Products
Reviews
Biological Activity Technical Data Background Product Datasheets Calculators

Biological Activity

BMS 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.

Technical Data

M.Wt:
593.66
Formula:
C28H34F3N5O4S
Solubility:
Soluble to 100 mM in DMSO and to 10 mM in ethanol
Purity:
≥98%
Storage:
Store at +4°C
CAS No:
445479-97-0

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.

Background References

  1. Effect of CCR2 inhibitor-loaded lipid micelles on inflammatory cell migration and cardiac function after myocardial infarction
    J Wang, MJ Seo, MB Deci, BR Weil, JM Canty, J Nguyen
    Int J Nanomedicine, 2018;13(0):6441-6451.
  2. CCR2(-) and CCR2(+) corneal macrophages exhibit distinct characteristics and balance inflammatory responses after epithelial abrasion
    J Liu, Y Xue, D Dong, C Xiao, C Lin, H Wang, F Song, T Fu, Z Wang, J Chen, H Pan, Y Li, D Cai, Z Li
    Mucosal Immunol, 2017;0(0):.
  3. CCR2 acts as scavenger for CCL2 during monocyte chemotaxis.
    Volpe S, Cameroni E, Moepps B
    PLoS ONE, 2012;7(5):e37208.
  4. Minocycline, a microglial inhibitor, blocks spinal CCL2-induced heat hyperalgesia and augmentation of glutamatergic transmission in substantia gelatinosa neurons.
    Huang C, Chen Y, Li A, Lu J, Wang H
    J Neuroinflammation, 2014;11(0):7.
  5. Discovery of disubstituted cyclohexanes as a new class of CC chemokine receptor 2 antagonists.
    Cherney et al.
    J.Med.Chem., 2008;51:721
  6. CCR2 receptor ligands inhibit Cav3.2 T-type calcium channels.
    You et al.
    Mol.Pharmacol., 2010;77:211

Product Datasheets

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Citations for BMS CCR2 22

The citations listed below are publications that use Tocris products. Selected citations for BMS CCR2 22 include:

4 Citations: Showing 1 - 4

  1. Regulation of CCL2 by EZH2 affects tumor-associated macrophages polarization and infiltration in breast cancer.
    Authors: Wang Et al.
    Cell Death Dis  2022;13:748
  2. Effect of CCR2 inhibitor-loaded lipid micelles on inflammatory cell migration and cardiac function after myocardial infarction.
    Authors: Wang Et al.
    Int J Nanomedicine  2018;13:6441
  3. M-sec regulates polarized secretion of inflammatory endothelial chemokines and facilitates CCL2-mediated lymphocyte transendothelial migration.
    Authors: Barzilai Et al.
    J Leukoc Biol  2016;99:1045
  4. CCR2 acts as scavenger for CCL2 during monocyte chemotaxis.
    Authors: Volpe Et al.
    PLoS One  2012;7:e37208

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