CCR2 Antagonist CAS: 445479-97-0
CCR2 Antagonist is A highly potent CKR-2B (CCR2) receptor antagonist.

CCR2 Antagonist (CAS 445479-97-0)

CCR2 Antagonist | CAS 445479-97-0 is rated 5.0 out of 5 by 2.
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Alternate Names: CC Chemokine Receptor 2 Antagonist
Application: CCR2 Antagonist is A highly potent CKR-2B (CCR2) receptor antagonist
CAS Number: 445479-97-0
Purity: ≥97%
Molecular Weight: 593.7
Molecular Formula: C28H34F3N5O4S
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data (including water content).
Submit a review for this product and receive 15 CruzCredits

CCR2 Antagonist is a cell-permeable cis-diamidocyclohexyl urea compound with high affinity binding to CKR-2B (chemokine receptor 2; CCR2), also designated CD192. CKR-2B is a G protein-coupled receptor with a unique conserved glutamic acid residue in transmembrane 7, Glu291. Research shows that this conserved residue is a critical site for small molecule antagonist binding. MCP-1 (chemokine ligand 2; CCL2) is a specific chemokine for the CKR-2B receptor and is responsible for recruiting monocytes, memory T cells, and dendritic cells to sites of tissue injury and infection. CCR2 Antagonist displays high affinity binding for CKR-2B ( IC50 = 5.1 nM) and potent functional antagonism (calcium flux IC50 = 18 nM and chemotaxis IC50 = 1 nM). Although Glu291 is a key receptor residue for CKR-2B, CCR2 Antagonist studies show that this inhibitor is not reliant upon Glu291 for its affinity binding, rather a nearby site. CCR2 Antagonist exhibits preferential binding for CKR-2B over CKR-3 (CCR3).


References

1. Carr, M.W., et al. 1994. Proc. Natl. Acad. Sci. U.S.A. 91: 3652-3656. PMID: 8170963
2. Cherney, R.J., et al. 2008. J. Med. Chem. 51: 721-724. PMID: 18232650
3. Xia, M. and Sui, Z. 2009. Expert Opin Ther Pat. 19: 295-303. PMID: 19441905

Physical State :
Solid
Solubility :
Soluble in DMSO (100 mM), and ethanol (10 mM).
Storage :
Store at 4° C
Refractive Index :
n20D 1.59 (Predicted)
IC50 :
MCP-1 binding to CCR2: IC50 = 5.1 nM; MCP-1/CCR2-mediated PBMCs Ca+2 flux: IC50 = 18 nM; MCP-1/CCR2-mediated chemotaxis: IC50 = 1 nM
pK Values :
pKa: 12.59 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
57350027
SMILES :
CC(C)NC(=O)NC1=C(C=C(C=C1)C(F)(F)F)C(=O)NCC(=O)N[[email protected]@H]2CCCC[[email protected]@H]2NC(=O)C3=CC=C(C=C3)SC

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CCR2 Antagonist (CAS 445479-97-0) Product Citations

See how others have used CCR2 Antagonist (CAS 445479-97-0). Click on the entry to view the PubMed entry .

Citations 1 to 10 of 25 total

PMID: # 30894684  Bao, D.|Zhao, J.|Zhou, X.|Yang, Q.|Chen, Y.|Zhu, J.|Yuan, P.|Yang, J.|Qin, T.|Wan, S.|Xing, J.| et al. 2019. Oncogene. 38: 5007-5020.

PMID: # 30918133  Kim, HL.|Kim, NS.|Cho, HY.|Park, SJ.|Lee, CK.|Choi, I.|Lee, SW.| et al. 2019. Biol. Pharm. Bull. 42: 915-922.

PMID: # 30426599  Natsagdorj, A.|Izumi, K.|Hiratsuka, K.|Machioka, K.|Iwamoto, H.|Naito, R.|Makino, T.|Kadomoto, S.|Shigehara, K.|Kadono, Y.|Lin, WJ.|Maolake, A.|Mizokami, A.| et al. 2019. Cancer Sci. 110: 279-288.

PMID: # 28655771  Singh, NK. et al. 2017. J. Biol. Chem. 292: 14080-14091.

PMID: # 28424406  An, J. et al. 2017. Oncotarget. 8: 39230-39240.

PMID: # 28202513  Steinberg, SM.|Shabaneh, TB.|Zhang, P.|Martyanov, V.|Li, Z.|Malik, BT.|Wood, TA.|Boni, A.|Molodtsov, A.|Angeles, CV.|Curiel, TJ.|Whitfield, ML.|Turk, MJ.| et al. 2017. Cancer Res. 77: 1599-1610.

PMID: # 28045930  Macanas-Pirard, P.|Quezada, T.|Navarrete, L.|Broekhuizen, R.|Leisewitz, A.|Nervi, B.|Ramírez, PA.| et al. 2017. PLoS ONE. 12: e0168888.

PMID: # 26910914  Hwang, CJ.|Park, MH.|Hwang, JY.|Kim, JH.|Yun, NY.|Oh, SY.|Song, JK.|Seo, HO.|Kim, YB.|Hwang, DY.|Oh, KW.|Han, SB.|Hong, JT.| et al. 2016. Oncotarget. 7: 11984-99.

PMID: # 26014148  Xu, M.|Wang, S.|Qi, Y.|Chen, L.|Frank, JA.|Yang, XH.|Zhang, Z.|Shi, X.|Luo, J.| et al. 2016. Mol. Carcinog. 55: 1002-11.

PMID: # 26756352  Laurent, V. et al. 2016. Nature communications. 7: 10230.

Citations 1 to 10 of 25 total
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Rated 5 out of 5 by from Works great Works great - no issues.
Date published: 2015-10-28
Rated 5 out of 5 by from Kitagawa et al Kitagawa et al. (PubMed ID 15215179) used CCR2 antagonist to alleviate progressive fibrosis in diseased kidneys by reducing CCR2-mediated MCP-1 expression. -SCBT Publication Review
Date published: 2015-01-28
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