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227016
Sigma-AldrichCCR2 Antagonist - CAS 445479-97-0 - Calbiochem
The CCR2 Antagonist, also referenced under CAS 445479-97-0, controls the biological activity of CCR2.
More>>The CCR2 Antagonist, also referenced under CAS 445479-97-0, controls the biological activity of CCR2. Less<<
MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.
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Description
Overview
A cis-diamidocyclohexyl urea compound that potently competes against MCP-1 binding to CCR2 (IC50 = 5.1 nM) and effectively inhibits MCP-1/CCR2-mediated PBMCs Ca+2 flux and chemotaxis (IC50 = 18 and 1 nM, respectively), while showing much less effect against eotaxin binding to CCR3 (37% inhibition at 10 µM). Mutageneis analysis indicates CCR2 Thr292 is critical in maintaining the high affinity antagonist binding.
Catalogue Number
227016
Brand Family
Calbiochem®
Synonyms
2-((Isopropylaminocarbonyl)amino)-N-(2-((cis-2-((4-(methylthio)benzoyl)amino)cyclohexyl)amino)-2-oxoethyl)-5-(trifluoromethyl)-benzamide, CC Chemokine Receptor 2 Antagonist
CCR2 Antagonist - CAS 445479-97-0 - Calbiochem Certificates of Analysis
Title
Lot Number
227016
References
Reference overview
Cherney, R.J., et al. 2008. J. Med. Chem.51, 721.
Data Sheet
Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.
Revision
19-August-2011 JSW
Synonyms
2-((Isopropylaminocarbonyl)amino)-N-(2-((cis-2-((4-(methylthio)benzoyl)amino)cyclohexyl)amino)-2-oxoethyl)-5-(trifluoromethyl)-benzamide, CC Chemokine Receptor 2 Antagonist
Description
A cis-diamidocyclohexyl urea compound that potently competes against MCP-1 binding to CCR2 (IC50 = 5.1 nM) and effectively inhibits MCP-1/CCR2-mediated PBMCs Ca+2 flux and chemotaxis (IC50 = 18 and 1 nM, respectively), while showing much less effect against eotaxin binding to CCR3 (37% inhibition at 10 µM). Mutageneis analysis indicates CCR2 Thr292 is critical in maintaining the high affinity antagonist binding.
Form
White solid
Intert gas (Yes/No)
Packaged under inert gas
CAS number
445479-97-0
Chemical formula
C₂₈H₃₄F₃N₅O₄S
Structure formula
Purity
≥97% by HPLC (racemic mixture)
Solubility
DMSO (60 mg/ml) or Ethanol (6 mg/ml). Gentle warming, rapid stirring, and/or sonication may be required for complete solubilization.
Storage
Protect from light +2°C to +8°C Hygroscopic
Do Not Freeze
Ok to freeze
Special Instructions
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.