227016

CCR2 Antagonist

The CCR2 Antagonist, also referenced under CAS 445479-97-0, controls the biological activity of CCR2.

• Synonym(s): CCR2 Antagonist, 2-((Isopropylaminocarbonyl)amino)-N-(2-((cis-2-((4-(methylthio)benzoyl)amino)cyclohexyl)amino)-2-oxoethyl)-5-(trifluoromethyl)-benzamide, CC Chemokine Receptor 2 Antagonist
• Empirical Formula (Hill Notation): C₂₈H₃₄F₃N₅O₄S
• CAS Number: 445479-97-0
• Molecular Weight: 593.66
• UNSPSC Code: 12352200

Properties

• Quality Level: 100
• Assay: ≥97% (racemic mixture, HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; desiccated (hygroscopic); protect from light
• color: white
• solubility: ethanol: 6 mg/mL; DMSO: 60 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C

Description

General 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.

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Preparation Note

Gentle warming, rapid stirring, and/or sonication may be required for complete solubilization.

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Cherney, R.J., et al. 2008. J. Med. Chem.51, 721.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable